Journal articles: 'Heterocyclic chemistry; Cancer'

1

Mir, Reyaz Hassan, Roohi Mohi-ud-din, Taha Umair Wani, Mohammad Ovais Dar, Abdul Jaleel Shah, Bashir Lone, Chawla Pooja, and Mubashir Hussain Masoodi. "Indole: A Privileged Heterocyclic Moiety in the Management of Cancer." Current Organic Chemistry 25, no. 6 (March 26, 2021): 724–36. http://dx.doi.org/10.2174/1385272825666210208142108.

Full text

Abstract:

Heterocyclic are a class of compounds that are intricately entwined into life processes. Almost more than 90% of marketed drugs carry heterocycles. Synthetic chemistry, in turn, allocates a cornucopia of heterocycles. Among the heterocycles, indole, a bicyclic structure consisting of a six-membered benzene ring fused to a five-membered pyrrole ring with numerous pharmacophores that generate a library of various lead molecules. Due to its profound pharmacological profile, indole got wider attention around the globe to explore it fully in the interest of mankind. The current review covers recent advancements on indole in the design of various anti-cancer agents acting by targeting various enzymes or receptors, including (HDACs), sirtuins, PIM kinases, DNA topoisomerases, and σ receptors.

APA, Harvard, Vancouver, ISO, and other styles

2

Georghiou, Paris E. "Preface." Pure and Applied Chemistry 82, no. 9 (January 1, 2010): iv. http://dx.doi.org/10.1351/pac20108209iv.

Full text

Abstract:

The 22nd International Congress on Heterocyclic Chemistry (ICHC-22) was held 2-7 August 2009 in St. John's, Newfoundland and Labrador, Canada. St. John's, the capital of Canada's youngest Province, Newfoundland and Labrador, is also Canada’s oldest and North America’s most easterly city. The Conference was chaired by Prof. Mohsen Daneshtalab (School of Pharmacy, Memorial University of Newfoundland) and was organized by the School of Pharmacy and the Chemistry Department at Memorial University of Newfoundland.Approximately 260 participants from over 30 different countries attended. The scientific program consisted of 10 plenary lectures, 19 invited lectures, 52 short communications, and 115 posters. Prof. Samuel Danishefsky (Sloan-Kettering Institute for Cancer Research, Columbia University) was honored with the 2009 ISHC Senior Award in Heterocyclic Chemistry, and Prof. John Wood (Colorado State University) was the 2009 Katritzky Junior Award winner. A special symposium entitled "Focus on heterocycles in organic synthesis today and tomorrow" was held during the Congress as a tribute to Prof. Victor Snieckus (Queen's University, Kingston) for his research accomplishments and long-time contribution to the International Society of Heterocyclic Chemistry (ISHC).The five Congress themes were:- New Methods in Heterocyclic Chemistry- Biologically Active Heterocycles (Pharmaceuticals/Agrochemicals)- Heterocyclic Natural Products and their Analogues- Applications of Heterocycles in Organic Synthesis- Heterocycles in Materials ScienceBesides the collection of 9 papers that are based on the plenary and invited lectures included in this issue of Pure and Applied Chemistry, the ICHC-22 Book of Abstracts is available online and can be downloaded for free from http://www.ichc2009.ca/abstract_book.pdf in pdf format.ICHC-23 will be held in Glasgow, Scotland, 31 July to 5 August 2011 with the following five main themes of heterocyclic chemistry: synthetic methodology, natural products and complex molecule synthesis, materials, medicinal chemistry, and nanochemistry. The conference will be chaired by Prof. Colin Suckling (University of Strathclyde).The organizers are grateful to all who contributed to a successful scientific program, especially to the speakers and to our public and private sponsors: City of St. John's, Memorial University of Newfoundland, IUPAC, Thieme, Wiley-Blackwell, Elsevier, Taiho Pharmaceutical Co., ChemRoutres Corporation, and American Diagnostica, Inc.Paris E. GeorghiouConference Editor

APA, Harvard, Vancouver, ISO, and other styles

3

Grover, Parul, Monika Bhardwaj, Garima Kapoor, Lovekesh Mehta, Roma Ghai, and K. Nagarajan. "Advances on Quinazoline Based Congeners for Anticancer Potential." Current Organic Chemistry 25, no. 6 (March 26, 2021): 695–723. http://dx.doi.org/10.2174/1385272825666210212121056.

Full text

Abstract:

The heterocyclic compounds have a great significance in medicinal chemistry because they have extensive biological activities. Cancer is globally the leading cause of death and it is a challenge to develop appropriate treatment for the management of cancer. Continuous efforts are being made to find a suitable medicinal agent for cancer therapy. Nitrogencontaining heterocycles have received noteworthy attention due to their wide and distinctive pharmacological activities. One of the most important nitrogen-containing heterocycles in medicinal chemistry is ‘quinazoline’ that possesses a wide spectrum of biological properties. This scaffold is an important pharmacophore and is considered a privileged structure. Various substituted quinazolines displayed anticancer activity against different types of cancer. This review highlights the recent advances in quinazoline based molecules as anticancer agents. Several in-vitro and in-vivo models used along with the results are also included. A subpart briefing natural quinazoline containing anticancer compounds is also incorporated in the review.

APA, Harvard, Vancouver, ISO, and other styles

4

Foldesi, Tamas, Balazs Volk, and Matyas Milen. "A Review of 2,3-Benzodiazepine-related Compounds: Diazepines and 1,2,5- Triazepines Fused with Five-membered Nitrogen Heterocycles." Current Organic Synthesis 15, no. 6 (August 29, 2018): 729–54. http://dx.doi.org/10.2174/1570179415666180601101856.

Full text

Abstract:

Background: 2,3-Benzodiazepines represent an important class of biologically active compounds, some members of this family have reached the human clinical stage. With formal bioisosteric replacement of the benzene ring to five-membered nitrogen heterocycles, several new diazepine and 1,2,5-triazepine derivatives have been synthesized in the past 30 years. Objective: Investigations in the field of heterocyclic chemistry is very important, because there could be several new medicines among the newly synthesized heterocyclic ring systems, which could be used against several diseases which have no remedy yet, for example some types of cancer. The research on antibacterial compounds is also an important field because of spreading of multiresistant pathogens. This review aims to summarize the literature of certain 2,3-benzodiazepine analogues. Conclusion: After a brief historical introduction, various ring systems containing a 2,3-diazepine or a 1,2,5- triazepine ring condensed with five-membered nitrogen heterocycles are disclosed. First, pyrrole-fused compounds are introduced, followed by indole and carbazole derivatives. After that, diverse ring systems containing an imidazole ring are presented. The review is closed with the chemistry of some interesting triazole and tetrazole derivatives. Many of these compounds bear significant biological efficacy.

APA, Harvard, Vancouver, ISO, and other styles

5

Harith M. Al-ajely. "Synthesis and pharmaceutical applications of Oxazine compounds derived from Pyronic, Salicylic, Antharanilic acids and Phenols." International Journal of Science and Research Archive 2, no. 2 (May 30, 2021): 074–86. http://dx.doi.org/10.30574/ijsra.2021.2.2.0250.

Full text

Abstract:

It is well known from FDA reports that More than 75% of the heterocyclic compounds are drugs and 90 of heterocyclic compounds are cancer drugs. The nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. Most drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties, More over heterocyclic compounds are important class of organic chemistry due to their widely spread in nature. Also there are many route for their action and many mechanistic pathways for their preparation and different metabolic actions. This comes from the easily building or removal of any functional group within the molecules. Changing just on group cause to change the metabolic pathway of the drug action and site of attack of the desired target accordingly. This great characteristic value make them much more important in drug discovery programs of many researchers and also encouraged us and drew attentions of other researchers to develop new ways for their synthesis. As a result different pharmacological and medical applications. Oxazie compounds are sub branch of heterocyclic compounds. These compounds having two hetero atoms, Oxygen and nitrogen within their structures make them much more important toward therapeutic studies. We are here in our investigation will focus on the methodologies and the therapeutic action of the titled compounds as well as other various applications.

APA, Harvard, Vancouver, ISO, and other styles

6

Aly, Ashraf A., Alaa A. Hassan, Maysa M. Makhlouf, and Stefan Bräse. "Chemistry and Biological Activities of 1,2,4-Triazolethiones—Antiviral and Anti-Infective Drugs." Molecules 25, no. 13 (July 3, 2020): 3036. http://dx.doi.org/10.3390/molecules25133036.

Full text

Abstract:

Mercapto-substituted 1,2,4-triazoles are very interesting compounds as they play an important role in chemopreventive and chemotherapeutic effects on cancer. In recent decades, literature has been enriched with sulfur- and nitrogen-containing heterocycles which are used as a basic nucleus of different heterocyclic compounds with various biological applications in medicine and also occupy a huge part of natural products. Therefore, we shed, herein, more light on the synthesis of this interesting class and its application as a biologically active moiety. They might also be suitable as antiviral and anti-infective drugs.

APA, Harvard, Vancouver, ISO, and other styles

7

Giuglio-Tonolo, Alain G., Christophe Curti, Thierry Terme, and Patrice Vanelle. "A Survey of Synthetic Routes and Antitumor Activities for Benzo[g]quinoxaline-5,10-diones." Molecules 25, no. 24 (December 14, 2020): 5922. http://dx.doi.org/10.3390/molecules25245922.

Full text

Abstract:

Anthracycline antibiotics play an important role in cancer chemotherapy. The need to improve their therapeutic index has stimulated an ongoing search for anthracycline analogs with enhanced properties. This review aims to summarize the common synthetic approaches to benzo[g]quinoxaline-5,10-diones and their uses in heterocyclic chemistry. Because of the valuable biological activities of the 1,4-diazaanthraquinone compounds, a summary of the most promising heterocyclic quinones is provided together with their antitumor properties.

APA, Harvard, Vancouver, ISO, and other styles

8

Ghahsare, Aref G., Zahra S. Nazifi, and Seyed M. R. Nazifi. "Structure-Bioactivity Relationship Study of Xanthene Derivatives: A Brief Review." Current Organic Synthesis 16, no. 8 (January 20, 2020): 1071–77. http://dx.doi.org/10.2174/1570179416666191017094908.

Full text

Abstract:

: Over the last decades, several heterocyclic derivatives compounds have been synthesized or extracted from natural resources and have been tested for their pharmaceutical activities. Xanthene is one of these heterocyclic derivatives. These compounds consist of an oxygen-containing central heterocyclic structure with two more cyclic structures fused to the central cyclic compound. It has been shown that xanthane derivatives are bioactive compounds with diverse activities such as anti-bacterial, anti-fungal, anti-cancer, and anti-inflammatory as well as therapeutic effects on diabetes and Alzheimer. The anti-cancer activity of such compounds has been one of the main research fields in pharmaceutical chemistry. Due to this diverse biological activity, xanthene core derivatives are still an attractive research field for both academia and industry. This review addresses the current finding on the biological activities of xanthene derivatives and discussed in detail some aspects of their structure-activity relationship (SAR).

APA, Harvard, Vancouver, ISO, and other styles

9

Salotra, Riddhi, and Divya Utreja. "A Comprehensive Appraisal of Chalcones and Their Heterocyclic Analogs as Antimicrobial Agents." Current Organic Chemistry 24, no. 23 (December 28, 2020): 2755–81. http://dx.doi.org/10.2174/1385272824999200922090524.

Full text

Abstract:

Owing to the growing demand for compelling antimicrobial agents, chalcones and their heterocyclic derivatives have engrossed prodigious attention of medicinal chemists as an effective clinical template for the synthesis of such agents on account of their structural diversity and molecular flexibility. Chalcones are considered as a fortunate scaffold in the field of both synthetic as well as natural product chemistry. They are reflected as a remarkable section of logically occurring pharmacophores that possess a comprehensive scale of biological activities, such as anti-cancer, anti-malarial, anti-viral and anti-inflammatory, rendering them with a high degree of assortment and noble therapeutic profile. They act as a crucial intermediate for the synthesis of novel heterocyclic skeletons holding biodynamic behavior. This review emphasizes on different aspects of chalcones including their natural sources, recent synthetic methodologies and evaluation of their anti-microbial potential. It is expected as a persuasive compilation on chalcones that may benefit the experts to design potent and less toxic chalcone referents as medicinal agents.

APA, Harvard, Vancouver, ISO, and other styles

10

Sharma, Sachin, Gaurav Joshi, Sourav Kalra, Sandeep Singh, and Raj Kumar. "Synthetic Versus Enzymatic Pictet-Spengler Reaction: An Overview." Current Organic Synthesis 15, no. 7 (October 16, 2018): 924–39. http://dx.doi.org/10.2174/1570179415666180613084014.

Full text

Abstract:

Background: Pictet-Spengler reactions is an irreplaceable part of cyclization reaction leading to the formation of indispensable heterocyclic moieties including imidazole, benzoxazole, pyrrole, indole and others having immense biological and chemical significance. Researchers have explored this reaction using different types of catalysts and reactions conditions (including solvents, acids, etc.) to ensure the better selectivity, less reaction time and high product yields. A total of five Pictet-Spenglerases have been discovered from various sources including plants, animals, fungi, and microbes, and are responsible for the synthesis of various important alkaloids of biological medicinal importance. Objective: The present review is a strenuous effort to assemble information mainly focusing on synthetic as well as biological Pictet-Spengler reactions catalysed by enzymes called Pictet-Spenglerase. Conclusion: In the present review, the recent advances in the PS-mediated synthesis of diverse heterocycles such as tetrahydroisoquinoline, tetrahydro-β-carbolines, tetrahydroimidazopyridines and other fused heterocycles via chemical as well as enzymatic pathways have been covered. The compounds find their scope as medicinal agents for the treatment of cancer, tuberculosis, bacterial infection, leishmanial, etc. The compilation is expected to provide a mechanistic insight to chemists to enhance the reaction condition, yields and another parameter to ensure the safe and inexpensive reaction conditions considering the “Green-Concept” of chemistry.

APA, Harvard, Vancouver, ISO, and other styles

11

Soni, Jay, Ayushi Sethiya, Nusrat Sahiba, Dinesh K. Agarwal, and Shikha Agarwal. "Contemporary Progress in the Synthetic Strategies of Imidazole and its Biological Activities." Current Organic Synthesis 16, no. 8 (January 20, 2020): 1078–104. http://dx.doi.org/10.2174/1570179416666191007092548.

Full text

Abstract:

: Heterocyclic compounds are pervasive in many areas of life and one of the heterocycles, imidazole is a unique heterocyclic five-membered aromatic compound having two sp2 hybridized nitrogen atoms. Its integral name is 1, 3 diazole and previously, it was known as glyoxalin. This moiety has achieved a considerable place among scientists in recent years by reason of its divergent synthetic strategies and uncommon biological and pharmacological activities, for example, anti-convulsant, anti-microbial, anti-cancer, anti-inflammatory, anti-tumor, anti-viral, anti-ulcer, analgesic, etc. Due to distinct therapeutic actions, it is still an engrossed area of research. Researchers currently are inventing new greener methods to synthesize its derivatives and to improve its pharmacological activities. The purpose of this review is to study the literature that can help researchers to explore this area, its prevailing program for synthesis in environmentally friendly conditions and biological profile throughout past decades.

APA, Harvard, Vancouver, ISO, and other styles

12

Matiadis, Dimitris, and Marina Sagnou. "Pyrazoline Hybrids as Promising Anticancer Agents: An Up-to-Date Overview." International Journal of Molecular Sciences 21, no. 15 (July 31, 2020): 5507. http://dx.doi.org/10.3390/ijms21155507.

Full text

Abstract:

Pyrazolines are five-membered heterocycles possessing two adjacent nitrogens. They have attracted significant attention from organic and medicinal chemists due to their potent biological activities and the numerous possibilities for structural diversification. In the last decade, they have been intensively studied as targets for potential anticancer therapeutics, producing a steady yearly rise in the number of published research articles. Many pyrazoline derivatives have shown remarkable cytotoxic activities in the form of heterocyclic or non-heterocyclic based hybrids, such as with coumarins, triazoles, and steroids. The enormous amount of related literature in the last 5 years prompted us to collect all these published data from screening against cancer cell lines, or protein targets like EGFR and structure activity relationship studies. Therefore, in the present review, a comprehensive account of the compounds containing the pyrazoline nucleus will be provided. The chemical groups and the structural modifications responsible for the activity will be highlighted. Moreover, emphasis will be given on recent examples from the literature and on the work of research groups that have played a key role in the development of this field.

APA, Harvard, Vancouver, ISO, and other styles

13

Dhuguru, Jyothi, and Rachid Skouta. "Role of Indole Scaffolds as Pharmacophores in the Development of Anti-Lung Cancer Agents." Molecules 25, no. 7 (April 1, 2020): 1615. http://dx.doi.org/10.3390/molecules25071615.

Full text

Abstract:

Lung cancer is the leading cause of death in men and women worldwide, affecting millions of people. Between the two types of lung cancers, non-small cell lung cancer (NSCLC) is more common than small cell lung cancer (SCLC). Besides surgery and radiotherapy, chemotherapy is the most important method of treatment for lung cancer. Indole scaffold is considered one of the most privileged scaffolds in heterocyclic chemistry. Indole may serve as an effective probe for the development of new drug candidates against challenging diseases, including lung cancer. In this review, we will focus on discussing the existing indole based pharmacophores in the clinical and pre-clinical stages of development against lung cancer, along with the synthesis of some of the selected anti-lung cancer drugs. Moreover, the basic mechanism of action underlying indole based anti-lung cancer treatment, such as protein kinase inhibition, histone deacetylase inhibition, DNA topoisomerase inhibition, and tubulin inhibition will also be discussed.

APA, Harvard, Vancouver, ISO, and other styles

14

Ali, Imran, Sofi Danish Mukhtar, Ming Fa Hsieh, Zeid A. Alothman, and Abdulrahman Alwarthan. "Facile synthesis of indole heterocyclic compounds based micellar nano anti-cancer drugs." RSC Advances 8, no. 66 (2018): 37905–14. http://dx.doi.org/10.1039/c8ra07060a.

Full text

APA, Harvard, Vancouver, ISO, and other styles

15

Anjaneyulu, Bendi, Sangeeta, and Naina Saini. "A Study on Camphor Derivatives and Its Applications: A Review." Current Organic Chemistry 25, no. 12 (July 14, 2021): 1404–28. http://dx.doi.org/10.2174/1385272825666210608115750.

Full text

Abstract:

Natural compounds are the prominent sources for the synthesis of abundant biologically active substances in medicinal chemistry. Camphor exists in two enantiomeric forms i.e., R and S, or both, which are readily obtainable. Camphor is a small molecule with chirality property that binds to some active site, together with its low cost and convenience to transform into synthetically useful derivatives and one of the most important monoterpenoids widely spread in plants and has been used as starting material for the various camphor based derivatives which exhibit several biological activities include antimicrobial, antiviral, antioxidant, analgesic and anti-cancer. Many of those simple derivatives are commercially available in the form of camphor sulfonic acid or ketopinic acid that can be easily be produced from camphor. This compound is primarily used as a chiral starting material in the enantiospecific synthesis of natural products is because of its available methods for the direct or indirect introduction of functionality at C-3, C-5, C-8, C-9, and C-10 carbon atoms. In this study, heterocyclic compounds derived from camphor are arranged in different groups as Camphor-Derived Simple Heterocycles, Fused Camphor-Derived Heterocycles, Spiro Camphor-Derived Heterocycles, Ring Expanded Camphor-Derived Heterocycles and Camphor derived metal complexes. This study summarizes the transformations of camphor and its derivatives along with their biological activities.

APA, Harvard, Vancouver, ISO, and other styles

16

Pandit, C., P. Dholaria, and K. Kapadiya. "Anticancer Evaluation of 1,5-Disubstituted Tetrazoles using Ugi-Azide Four-Component Reactions (UA-4CRs)." Asian Journal of Organic & Medicinal Chemistry 4, no. 4 (2019): 216–21. http://dx.doi.org/10.14233/ajomc.2019.ajomc-p204.

Full text

Abstract:

Azide isocyanide-based multicomponent reactions allow the formation of relatively complex molecules through a one-pot synthesis. The proposed reactions have been coupled of four classes of compounds including 3-phenoxybenzaldehyde, various aromatic amines, TMS-N3 and tertiary butylisocyanide, which is known as Ugi-azide four-component reactions (UA-4CRs). It generated a diverse class of 1,5-disubstituted tetrazoles which are an important drug-like scaffold known for their ability to mimic the carcinogenic conformers used in medicinal chemistry. This work presents a concise, novel, general strategy to access a surplus of new heterocyclic scaffolds through the Ugi-azide reaction. Frequency in anticancer drug design can be partly attributed to their being extremely common in nature and there are multiple metabolic pathways and cellular processes within cancer pathology that can be susceptible to heterocycles-based drugs. The anticancer screening of derived molecules were carried out using one dose response study using NCI-60 cell-lines and found most active in breast cancer cell-lines

APA, Harvard, Vancouver, ISO, and other styles

17

Omar, Rebaz, Pelin Koparir, and Metin Koparir. "SYNTHESIS OF 1,3-THIAZOLE DERIVATIVES." INDIAN DRUGS 58, no. 01 (April 30, 2021): 7–19. http://dx.doi.org/10.53879/id.58.01.12427.

Full text

Abstract:

Many heterocyclic compounds containing nitrogen atom are used in drug development. Thiazole is one of the most important heterocyclic compounds in drug design, which contains sulfur and nitrogen atom. Different site reactions in thiazole compounds extend to new drug synthesis and plays an important role in medicinal chemistry. Thiazole and derivatives are found to possess widely biological activities such as anti-inflammatory, anti-diabetic, anti-microbial, anti-cancer, anti-consulsant, anti-HIV, anti-hypertensive, anti-Alzheimer, anti-oxidant and anthelmintic. The aim of this review is to corroborate procedures which are available for the synthesis 1,3-thiazole derivatives

APA, Harvard, Vancouver, ISO, and other styles

18

Gazizov, Almir S., Andrey V. Smolobochkin, Elizaveta A. Kuznetsova, Dinara S. Abdullaeva, Alexander R. Burilov, Michail A. Pudovik, Alexandra D. Voloshina, et al. "The Highly Regioselective Synthesis of Novel Imidazolidin-2-Ones via the Intramolecular Cyclization/Electrophilic Substitution of Urea Derivatives and the Evaluation of Their Anticancer Activity." Molecules 26, no. 15 (July 22, 2021): 4432. http://dx.doi.org/10.3390/molecules26154432.

Full text

Abstract:

A series of novel 4-(het)arylimidazoldin-2-ones were obtained by the acid-catalyzed reaction of (2,2-diethoxyethyl)ureas with aromatic and heterocyclic C-nucleophiles. The proposed approach to substituted imidazolidinones benefits from excellent regioselectivity, readily available starting materials and a simple procedure. The regioselectivity of the reaction was rationalized by quantum chemistry calculations and control experiments. The anti-cancer activity of the obtained compounds was tested in vitro.

APA, Harvard, Vancouver, ISO, and other styles

19

Bhat, Mahesh, and Shiddappa Lagamappa Belagali. "Structural Activity Relationship and Importance of Benzothiazole Derivatives in Medicinal Chemistry: A Comprehensive Review." Mini-Reviews in Organic Chemistry 17, no. 3 (April 28, 2020): 323–50. http://dx.doi.org/10.2174/1570193x16666190204111502.

Full text

Abstract:

:Benzothiazole (1, 3-benzothiazole) is one of the heterocyclic compounds, which is a weak base having varied biological activities. The unique methine center present in the thiazole ring makes benzothiazole as the most important heterocyclic compound. It is a common and integral structure of many natural and synthetic bioactive molecules. Benzothiazole derivatives show a variety of activities, with less toxic effects and their derivatives showed enhanced activities, which has proven Benzothiazole scaffold as one of the important moieties in medicinal chemistry. Benzothiazole ring containing compounds possess various pharmacological activities such as anti-viral, anti-microbial, antiallergic, anti-diabetic, anti-tumor, anti-inflammatory, anthelmitic and anti-cancer, which makes benzothiazole a rapidly developing and interesting compound in the medicinal chemistry. This review briefly explains the importance, common methods of synthesis of the benzothiazole scaffold and also explains the popular benzothiazole molecules which have applications in various fields of chemistry. A review has been carried out based on various pharmacological activities containing benzothiazole moieties and rationalize the activities based on the structural variations. Literature on benzothiazole derivatives reveals that substitution on the C-2 carbon atom and C-6 are the reasons for a variety of biological activities.

APA, Harvard, Vancouver, ISO, and other styles

20

Holmes, Jordan, Rachel J. Kearsey, Katie A. Paske, Frances N. Singer, Suliman Atallah, Christopher M. Pask, Roger M. Phillips, and Charlotte E. Willans. "Tethered N-Heterocyclic Carbene-Carboranyl Silver Complexes for Cancer Therapy." Organometallics 38, no. 12 (June 7, 2019): 2530–38. http://dx.doi.org/10.1021/acs.organomet.9b00228.

Full text

APA, Harvard, Vancouver, ISO, and other styles

21

Abdelrehim, El-sayed M., and Doaa S. El-Sayed. "A New Synthesis of Poly Heterocyclic Compounds Containing [1,2,4]triazolo and [1,2,3,4]tetrazolo Moieties and their DFT Study as Expected Anti-cancer Reagents." Current Organic Synthesis 17, no. 3 (June 9, 2020): 211–23. http://dx.doi.org/10.2174/1570179417666200226092516.

Full text

Abstract:

Background: 2-amino-3-cyanopyridines are good starting reagents that have been used in synthesis of many heterocyclic compounds such as pyridopyrimidines, [1,2,4]triazolo and [1,2,3,4] tetrazolo derivatives which have biological activities as anti-microbial and cytotoxic activities. Meanwhile [1,2,4]triazolo and [1,2,3,4]tetrazolo derivatives are well known to possess many physiological activities, such as anticancer , antifungal, muscle relaxant, hypnotic, anti-inflammatory, diuretic and antihypertensive activities. A broad class of heterocyclic compounds has been studied to demonstrate their biological activity on the structures of DNA and RNA. Several of important functions make Tankyrases acts as targets in potential drug. Objective: The article focuses on synthesis of [1,2,4]triazolo and [1,2,3,4]tetrazolo derivatives and their theoretical calculations that suggest they are anti-cancer substances. Materials and Methods: DFT and computational studies were performed on the structural properties of experimental molecules experimentally, and significant theoretical calculations were performed based on density functional theory (DFT) with Becke’s three-parameter exchange function21-22 of correlation functional Lee Yang Parr (B3LYP) with the basis set 6-31G (d,p) using Gaussian 03 software23. Geometrical parameters of the optimized structures were calculated and also the charge on each atom (Mulliken charge). Chemcraft program24 was used to visualize the optimized structure and ChemBio3D ultra 12.0 was used to visualize the highest occupied and lowest unoccupied molecular orbitals. Results: Preliminary screening in five studied ligands acts as inhibitors for different active sites along the target. The molecular docking study also revealed that the compound 6c was the most effective compounds in inhibiting Tankyrase I enzyme (2rf5), this result can help strongly in inhibition of carcinogenic cells and cancer treatment. Conclusion: We have described a new practical cyclocondensation synthesis for a series of [1,2,4]triazolo[4,3- c]pyrido[3,2-e] pyrimidine and pyrido[2',3':4,5] pyrimido[6,1-c][1,2,4] triazine from 2-amino-3-cyano-4.6- diarylpyridines. Also polyheterocyclic compounds containing [1,2,4]triazolo and [1,2,3,4]tetrazolo moieties were also synthesized through the reactions of 3-hydrazino-8,10-diaryl [1,2,4]triazolo[4,3-c]pyrido[3,2- e]pyrimidine with both formic acid and the formation of diazonuim salt respectively. Newly synthesized heterocycles structures were confirmed using elemental analysis, IR, 1H-NMR, 13C-NMR and mass spectral data. DFT and computational studies were carried out on five of the synthesized poly heterocyclic compounds to show their structural and geometrical parameters involved in the study. Molecular docking using Tankyrase I enzyme as a target showed how the studied heterocyclic compounds act as a ligand interacting most of active sites on Tankyrase I with a type of interactions specified for H-bonding and VDW. We investigated that the five studied ligands act as inhibitors for different active sites along the target. The molecular docking study also revealed that the compound 6c was the most effective compounds in inhibiting Tankyrase I enzyme (2rf5), this result can help strongly in inhibition of carcinogenic cells and cancer treatment.

APA, Harvard, Vancouver, ISO, and other styles

22

Al Nasr, Ibrahim, Nedra Touj, Waleed Koko, Tariq Khan, Ismail Özdemir, Sedat Yaşar, and Naceur Hamdi. "Biological Activities of NHC–Pd(II) Complexes Based on Benzimidazolylidene N-heterocyclic Carbene (NHC) Ligands Bearing Aryl Substituents." Catalysts 10, no. 10 (October 15, 2020): 1190. http://dx.doi.org/10.3390/catal10101190.

Full text

Abstract:

N-heterocyclic carbene (NHC) precursors (2a–i), their pyridine-enhanced precatalyst preparation stabilization and initiation (PEPPSI)-themed palladium N-heterocyclic carbene complexes (3a–i) and palladium N-heterocyclic triphenylphosphines complexes (4a–i) were synthesized and characterized by elemental analysis and 1H NMR, 13C NMR, IR, and LC–MS spectroscopic techniques. The (NHC)Pd(II) complexes 3–4 were tested against MCF7 and MDA-MB-231 cancer cells, Escherichia coli, methicillin-resistant Staphylococcus aureus (MRSA), Candida albicans microorganisms, Leishmania major promastigotes and amastigotes, Toxoplasma gondii parasites, and Vero cells in vitro. The biological assays indicated that all compounds are highly active against cancer cells, with an IC50 < 1.5 µg mL−1. Eight compounds proved antibacterial and antileishmanial activities, while only three compounds had strong antifungal activities against C. albicans. In our conclusion, compounds 3 (b, f, g, and h) and 4b are the most suitable drug candidates for anticancer, antimicrobial, and antiparasitical.

APA, Harvard, Vancouver, ISO, and other styles

23

Kletskov, Alexey V., Nikolay A. Bumagin, Fedor I. Zubkov, Dmitry G. Grudinin, and Vladimir I. Potkin. "Isothiazoles in the Design and Synthesis of Biologically Active Substances and Ligands for Metal Complexes." Synthesis 52, no. 02 (October 17, 2019): 159–88. http://dx.doi.org/10.1055/s-0039-1690688.

Full text

Abstract:

The chemistry of isothiazoles is being intensively developed, which is evidenced by the wide range of selective transformations involving the isothiazole heterocycle and the high biological activity of its derivatives that can be used as effective new drugs and plant protection chemicals. Some representatives of isothiazoles have proven to be synergists of bioactive substances, which opens the way to lower the doses of drugs used and is especially important in cancer chemotherapy. In the framework of the present review, the accomplishments in the chemistry of isothiazoles over the past 18 years are examined, whilst current strategies for the synthesis of isothiazole-containing molecules and key directions of studies in this field of heterocyclic chemistry are discussed. Considerable attention is paid to chlorinated isothiazoles and strategies for their use in the synthesis of biologically active substances. In addition, a comprehensive review of existing literature in the field of metal complexes of isothiazoles is given, including the results and prospects for the practical use of isothiazole–metal complexes as catalysts for cross-coupling reactions in aqueous and aqueous–alcoholic media (‘green chemistry’).1 Introduction2 Synthesis by Ring-Forming Reactions2.1 Intramolecular Cyclization2.2 (4+1)-Heterocyclization2.3 (3+2)-Heterocyclization2.4 Syntheses by Ring Transformations3 Isothiazoles by Ring Functionalization Reactions: Nucleophilic Substitution, Cross-Coupling and Side-Chain Functionalization4 Selected Syntheses of Biologically Active Isothiazole Derivatives5 Isothiazoles in the Synthesis of Transition-Metal Complexes and in Metal-Complex Catalysis6 Conclusion

APA, Harvard, Vancouver, ISO, and other styles

24

Rodrigues, Fiona C., N. V. Anil Kumar, Gangadhar Hari, K. S. R. Pai, and Goutam Thakur. "The inhibitory potency of isoxazole-curcumin analogue for the management of breast cancer: A comparative in vitro and molecular modeling investigation." Chemical Papers 75, no. 11 (July 12, 2021): 5995–6008. http://dx.doi.org/10.1007/s11696-021-01775-9.

Full text

Abstract:

AbstractCurcumin, a potent phytochemical derived from the spice element turmeric, has been identified as a herbal remedy decades ago and has displayed promise in the field of medicinal chemistry. However, multiple traits associated with curcumin, such as poor bioavailability and instability, limit its effectiveness to be accepted as a lead drug-like entity. Different reactive sites in its chemical structure have been identified to incorporate modifications as attempts to improving its efficacy. The diketo group present in the center of the structural scaffold has been touted as the group responsible for the instability of curcumin, and substituting it with a heterocyclic ring contributes to improved stability. In this study, four heterocyclic curcumin analogues, representing some broad groups of heterocyclic curcuminoids (isoxazole-, pyrazole-, N-phenyl pyrazole- and N-amido-pyrazole-based), have been synthesized by a simple one-pot synthesis and have been characterized by FTIR, 1H-NMR, 13C-NMR, DSC and LC–MS. To predict its potential anticancer efficacy, the compounds have been analyzed by computational studies via molecular docking for their regulatory role against three key proteins, namely GSK-3β—of which abnormal regulation and expression is associated with cancer; Bcl-2—an apoptosis regulator; and PR which is a key nuclear receptor involved in breast cancer development. One of the compounds, isoxazole-curcumin, has consistently indicated a better docking score than the other tested compounds as well as curcumin. Apart from docking, the compounds have also been profiled for their ADME properties as well as free energy binding calculations. Further, the in vitro cytotoxic evaluation of the analogues was carried out by SRB assay in breast cancer cell line (MCF7), out of which isoxazole-curcumin (IC50–3.97 µM) has displayed a sevenfold superior activity than curcumin (IC50–21.89 µM). In the collation of results, it can be suggested that isoxazole-curcumin behaves as a potential lead owing to its ability to be involved in a regulatory role with multiple significant cancer proteins and hence deserves further investigations in the development of small molecule-based anti-breast cancer agents. Graphic abstract

APA, Harvard, Vancouver, ISO, and other styles

25

Gong, Guo-Hua, Ming Bian, Chun-Yan Liu, and Bin Zhang. "Heterocyclic pyran and polyhydroquinoline derivatives to inhibit human breast cancer cells." Main Group Chemistry 18, no. 1 (March 4, 2019): 15–22. http://dx.doi.org/10.3233/mgc-180676.

Full text

APA, Harvard, Vancouver, ISO, and other styles

26

Mir, Shafia, Ayaz Mahmood Dar, and Bashir Ahmad Dar. "Synthetic Strategies of Benzothiazines: A Mini Review." Mini-Reviews in Organic Chemistry 17, no. 2 (February 28, 2020): 148–57. http://dx.doi.org/10.2174/1570193x16666181206101439.

Full text

Abstract:

Benzothiazine is a heterocyclic compound consisting of a benzene ring attached to the 6- membered thiazine ring. The benzothiazines constitute the group of heterocyclic compounds as they have found a variety of industrial uses and show promise as herbicides. Besides this, benzothiazines play an important role in the field of drug discovery as they have the potential to act as drug candidates for the treatment of a large number of diseases including, cancer, vasorelaxant, diabetic, hypertension, mycotic infection and microbial infection. The presence of nitrogen-sulphur axis and similarity in the structure with phenothiazine drugs help the benzothiazines to act as drugs for the treatment of a number of diseases. Herein, we represent different synthetic strategies for the simple and multi-component synthesis of benzothiazine heterocyclic derivatives. The strategies mostly involve the use of 2-aminothiophenol, 1, 3-dicarbonyl compounds or α-haloketones. In almost all the strategies, the potential yields have been obtained.

APA, Harvard, Vancouver, ISO, and other styles

27

Adel, Mai, Rabah Serya, Deena Lasheen, and Khaled Abouzid. "Pyrrolopyrimidine, A Multifaceted Scaffold in Cancer Targeted Therapy." Drug Research 68, no. 09 (February 12, 2018): 485–98. http://dx.doi.org/10.1055/s-0044-101256.

Full text

Abstract:

AbstractPyrrolopyrimidine derivatives represent a class of biologically active heterocyclic compounds which can serve as promising scaffolds that display remarkable biological activities, such as anti-inflammatory, antimicrobial, antiviral and anticancer. In the last few years, several pyrrolopyrimidine derivatives have been approved by the US FDA and in other countries for the treatment of different diseases or are currently in phase I/II clinical trials. Due to their inimitable antioxidant and anti-tumor properties, researchers were inspired to develop novel derivatives for the treatment of different types of cancer. The present review summarizes recent literature up to 2017 on the most recent development in the medicinal chemistry of pyrrolopyrimidine derivatives and their potential as anticancer therapeutics, especially compounds acting as kinase inhibitors.

APA, Harvard, Vancouver, ISO, and other styles

28

Holenya, Pavlo, Suzan Can, Riccardo Rubbiani, Hamed Alborzinia, Anja Jünger, Xinlai Cheng, Ingo Ott, and Stefan Wölfl. "Detailed analysis of pro-apoptotic signaling and metabolic adaptation triggered by a N-heterocyclic carbene–gold(i) complex." Metallomics 6, no. 9 (2014): 1591–601. http://dx.doi.org/10.1039/c4mt00075g.

Full text

APA, Harvard, Vancouver, ISO, and other styles

29

Wardakhan, Wagnat W., and Eman M. Samir. "The Reaction of Cyclopentanone with Cyanomethylene Reagents: Novel Synthesis of Pyrazole, Thiophene, and Pyridazine Derivatives." Journal of Chemistry 2013 (2013): 1–10. http://dx.doi.org/10.1155/2013/427158.

Full text

Abstract:

The reaction of cyclopentanone with either malononitrile or ethyl cyanoacetate gave the corresponding condensated products. The latter underwent some heterocyclic reactions to give new pyrazole, thiophene, and pyridazine derivatives. The antitumor evaluation of the newly synthesized products against the three cancer cells, namely, breast adenocarcinoma (MCF-7), nonsmall cell lung cancer (NCI-H460), and CNS cancer (SF-268) showed that some of them have high inhibitory effect towards three cell lines which is higher than the standard.

APA, Harvard, Vancouver, ISO, and other styles

30

Andreani, Aldo, Massimiliano Granaiola, Alberto Leoni, Alessandra Locatelli, Rita Morigi, Mirella Rambaldi, Gianluca Giorgi, and Laura Salvini. "Cancer fighting cancer: synthesis of the new heterocyclic system diimidazo[1,2-a:1,2-c]pyrimidine." Arkivoc 2002, no. 11 (November 11, 2002): 32–38. http://dx.doi.org/10.3998/ark.5550190.0003.b04.

Full text

APA, Harvard, Vancouver, ISO, and other styles

31

Alho, Daniela, Jorge Salvador, Marta Cascante, and Silvia Marin. "Synthesis and Antiproliferative Activity of Novel Heterocyclic Glycyrrhetinic Acid Derivatives." Molecules 24, no. 4 (February 20, 2019): 766. http://dx.doi.org/10.3390/molecules24040766.

Full text

Abstract:

A new series of glycyrrhetinic acid derivatives has been synthesized via the introduction of different heterocyclic rings conjugated with an α,β-unsaturated ketone in its ring A. These new compounds were screened for their antiproliferative activity in a panel of nine human cancer cell lines. Compound 10 was the most active derivative, with an IC50 of 1.1 µM on Jurkat cells, which is 96-fold more potent than that of glycyrrhetinic acid, and was 4-fold more selective toward that cancer cell line. Further biological studies performed in Jurkat cells showed that compound 10 is a potent inducer of apoptosis that activates both the intrinsic and extrinsic pathways.

APA, Harvard, Vancouver, ISO, and other styles

32

Amr, Abd El-Galil E., Hassan Z. Ghanem, Mohamed A. Al-Omar, Mohamed M. Abdalla, Mohamed G. Assy, and Islam Ragab. "Anti-Cancer and Kinases Inhibitor Activities of Synthesized Heterocyclic Substituted Thiophene Fused with Cyclohexane Derivatives." Journal of Computational and Theoretical Nanoscience 14, no. 1 (January 1, 2017): 768–74. http://dx.doi.org/10.1166/jctn.2017.6271.

Full text

Abstract:

We herein report the anti-cancer and kinases inhibitor activities of some synthesized heterocyclic substituted thiophene fused with cyclohexane derivatives (Fig. 1) were synthesized before. Sixteen of these compounds were conveniently screened for their in vitro cytotoxicity against a wide range of cell lines, and showed potent activities against lung and leukemic cancer cell lines. The in vivo antilung and antileukemic cancers of the most active in vitro compounds was estimated and founded highly potent and compared to the standard drugs Bevacizumab and Etoposide. In search for the mechanism of action of anticancer activities it was found that these compounds exert its action via sphingosine kinase inhibition and inhibition of p53 ubiquitination.

APA, Harvard, Vancouver, ISO, and other styles

33

Mishra, Abhinav Prasoon, Ankit Bajpai, and Awani Kumar Rai. "1,4-Dihydropyridine: A Dependable Heterocyclic Ring with the Promising and the Most Anticipable Therapeutic Effects." Mini-Reviews in Medicinal Chemistry 19, no. 15 (September 4, 2019): 1219–54. http://dx.doi.org/10.2174/1389557519666190425184749.

Full text

Abstract:

: Nowadays, heterocyclic compounds act as a scaffold and are the backbone of medicinal chemistry. Among all of the heterocyclic scaffolds, 1,4-Dihydropyridine (1,4-DHP) is one of the most important heterocyclic rings that possess prominent therapeutic effects in a very versatile manner and plays an important role in synthetic, medicinal, and bioorganic chemistry. The main aim of the study is to review and encompass relevant studies related to 1,4-DHP and excellent therapeutic benefits of its derivatives. An extensive review of Pubmed-Medline, Embase and Lancet’s published articles was done to find all relevant studies on the activity of 1,4-DHP and its derivatives. 1,4-DHP is a potent Voltage-Gated Calcium Channel (VGCC) antagonist derivative which acts as an anti-hypertensive, anti- anginal, anti-tumor, anti-inflammatory, anti-tubercular, anti-cancer, anti-hyperplasia, anti-mutagenic, anti-dyslipidemic, and anti-ulcer agent. From the inferences of the study, it can be concluded that the basic nucleus, 1,4-DHP which is a voltage-gated calcium ion channel blocker, acts as a base for its derivatives that possess different important therapeutic effects. There is a need of further research of this basic nucleus as it is a multifunctional moiety, on which addition of different groups can yield a better drug for its other activities such as anti-convulsant, anti-oxidant, anti-mutagenic, and anti-microbial. This review would be significant for further researches in the development of several kinds of drugs by representing successful matrix for the medicinal agents.

APA, Harvard, Vancouver, ISO, and other styles

34

Liu, Xu, Xiao-Jing Pang, Yuan Liu, Wen-Bo Liu, Yin-Ru Li, Guang-Xi Yu, Yan-Bing Zhang, Jian Song, and Sai-Yang Zhang. "Discovery of Novel Diarylamide N-Containing Heterocyclic Derivatives as New Tubulin Polymerization Inhibitors with Anti-Cancer Activity." Molecules 26, no. 13 (July 2, 2021): 4047. http://dx.doi.org/10.3390/molecules26134047.

Full text

Abstract:

Tubulin has been regarded as an attractive and successful molecular target in cancer therapy and drug discovery. Vicinal diaryl is a simple scaffold found in many colchicine site tubulin inhibitors, which is also an important pharmacophoric point of tubulin binding and anti-cancer activity. As the continuation of our research work on colchicine binding site tubulin inhibitors, we designed and synthesized a series of diarylamide N-containing heterocyclic derivatives by the combination of vicinal diaryl core and N-containing heterocyclic skeletons into one hybrid though proper linkers. Among of these compounds, compound 15b containing a 5-methoxyindole group exhibited the most potent inhibitory activity against the tested three human cancer cell lines (MGC-803, PC-3 and EC-109) with IC50 values of 1.56 μM, 3.56 μM and 14.5 μM, respectively. Besides, the SARs of these compounds were preliminarily studied and summarized. The most active compound 15b produced the inhibition of tubulin polymerization in a dose-dependent manner and caused microtubule network disruption in MGC-803 cells. Therefore, compound 15b was identified as a novel tubulin polymerization inhibitor targeting the colchicine binding site. In addition, the results of molecular docking also suggested compound 15b could tightly bind into the colchicine binding site of β-tubulin.

APA, Harvard, Vancouver, ISO, and other styles

35

Slimani, Ichraf, Serap Şahin-Bölükbaşı, Mustafa Ulu, Enes Evren, Nevin Gürbüz, İlknur Özdemir, Naceur Hamdi, and İsmail Özdemir. "Rhodium(i) N-heterocyclic carbene complexes: synthesis and cytotoxic properties." New Journal of Chemistry 45, no. 11 (2021): 5176–83. http://dx.doi.org/10.1039/d1nj00144b.

Full text

Abstract:

A series of benzimidazolium salts and their [RhCl(NHC)(COD)] complexes were synthesized. All compounds were screened for in vitro cytotoxic activities against a panel of human cancer cells (HT-29 colon, Ishikawa endometrial, U-87 glioblastoma) using the MTT assay for 48 h incubation time.

APA, Harvard, Vancouver, ISO, and other styles

36

Mahalingam, Viswanathan, Nataraj Chitrapriya, Frank R. Fronczek, and Karuppannan Natarajan. "New Ru(II)–dmso complexes with heterocyclic hydrazone ligands towards cancer chemotherapy." Polyhedron 27, no. 7 (May 2008): 1917–24. http://dx.doi.org/10.1016/j.poly.2008.02.036.

Full text

APA, Harvard, Vancouver, ISO, and other styles

37

González-Andrés, Paula, Laura Fernández-Peña, Carlos Díez-Poza, Carlos Villalobos, Lucía Nuñez, and Asunción Barbero. "Marine Heterocyclic Compounds That Modulate Intracellular Calcium Signals: Chemistry and Synthesis Approaches." Marine Drugs 19, no. 2 (January 31, 2021): 78. http://dx.doi.org/10.3390/md19020078.

Full text

Abstract:

Intracellular Ca2+ plays a pivotal role in the control of a large series of cell functions in all types of cells, from neurotransmitter release and muscle contraction to gene expression, cell proliferation and cell death. Ca2+ is transported through specific channels and transporters in the plasma membrane and subcellular organelles such as the endoplasmic reticulum and mitochondria. Therefore, dysregulation of intracellular Ca2+ homeostasis may lead to cell dysfunction and disease. Accordingly, chemical compounds from natural origin and/or synthesis targeting directly or indirectly these channels and proteins may be of interest for the treatment of cell dysfunction and disease. In this review, we show an overview of a group of marine drugs that, from the structural point of view, contain one or various heterocyclic units in their core structure, and from the biological side, they have a direct influence on the transport of calcium in the cell. The marine compounds covered in this review are divided into three groups, which correspond with their direct biological activity, such as compounds with a direct influence in the calcium channel, compounds with a direct effect on the cytoskeleton and drugs with an effect on cancer cell proliferation. For each target, we describe its bioactive properties and synthetic approaches. The wide variety of chemical structures compiled in this review and their significant medical properties may attract the attention of many different researchers.

APA, Harvard, Vancouver, ISO, and other styles

38

Iacopetta, Domenico, Jessica Ceramella, Camillo Rosano, Annaluisa Mariconda, Michele Pellegrino, Marco Sirignano, Carmela Saturnino, et al. "N-Heterocyclic Carbene-Gold(I) Complexes Targeting Actin Polymerization." Applied Sciences 11, no. 12 (June 18, 2021): 5626. http://dx.doi.org/10.3390/app11125626.

Full text

Abstract:

Transition metal complexes are attracting attention because of their various chemical and biological properties. In particular, the NHC-gold complexes represent a productive field of research in medicinal chemistry, mostly as anticancer tools, displaying a broad range of targets. In addition to the already known biological targets, recently, an important activity in the organization of the cell cytoskeleton was discovered. In this paper, we demonstrated that two NHC-gold complexes (namely AuL4 and AuL7) possessing good anticancer activity and multi-target properties, as stated in our previous studies, play a major role in regulating the actin polymerization, by the means of in silico and in vitro assays. Using immunofluorescence and direct enzymatic assays, we proved that both the complexes inhibited the actin polymerization reaction without promoting the depolymerization of actin filaments. Our outcomes may contribute toward deepening the knowledge of NHC-gold complexes, with the objective of producing more effective and safer drugs for treating cancer diseases.

APA, Harvard, Vancouver, ISO, and other styles

39

Verma, Tarawanti, Manish Sinha, and Nitin Bansal. "Heterocyclic Compounds Bearing Triazine Scaffold and Their Biological Significance: A Review." Anti-Cancer Agents in Medicinal Chemistry 20, no. 1 (April 10, 2020): 4–28. http://dx.doi.org/10.2174/1871520619666191028111351.

Full text

Abstract:

Benzene is a six-membered hydrocarbon ring system and if three carbon-hydrogen units of benzene ring are replaced by nitrogen atoms then triazine is formed. Triazines are present in three isomeric forms 1,2,3- triazine, 1,2,4-triazine, and 1,3,5-triazine according to the position of the nitrogen atom. These are weak bases having weaker resonance energy than benzene, so nucleophilic substitution is preferred than electrophilic substitution. Triazine is an interesting class of heterocyclic compounds in medicinal chemistry. Numerous synthetic derivatives of triazine have been prepared and evaluated for a wide spectrum of biological activities in different models with desired findings such as antibacterial, antifungal, anti-cancer, antiviral, antimalarial, antiinflammatory, antiulcer, anticonvulsant, antimicrobial, insecticidal and herbicidal agents. Triazine analogs have exposed potent pharmacological activity. So, triazine nucleus may be considered as an interesting core moiety for researchers for the development of future drugs.

APA, Harvard, Vancouver, ISO, and other styles

40

Anjana, V. S., and P. Manoj Kumar. "An Overview on Medicinal Perspective and Biological Behavior of Benzotriazole; Synthetic Study on Its Multifaceted Biological Activities." International Journal of Research and Review 8, no. 5 (June 2, 2021): 365–78. http://dx.doi.org/10.52403/ijrr.20210546.

Full text

Abstract:

Benzotriazole (BTA) is a nitrogen containing heterocyclic derivative containing three nitrogen atoms at 1st, 2nd and 3rd positions with chemical formula C6H5N3. Benzotriazole and its derivatives have great significance in medicinal chemistry and these derivatives were used by several chemists for therapeutic conditions because it possessing a wide spectrum of pharmacological activities including anti bacterial, anti fungal, anti viral, anti inflammatory, anti hyperglycemic, anti hypertensive, anti cancer and analgesic activity. In this review, different synthetic methods for the preparation of benzotriazole, importance of benzotriazole derivatives in biomedical research, highlighting its biological behavior, versatile activities and Structure Activity Relationship (SAR) studies are described. This review will help the researchers to understand the structure activity relationships and improvise the concepts in their research field. Keywords: Benzotriazole, Anti microbial, Anthelmintic, Analgesic, Anti mycobacterial, Anti viral, Anti oxidative, Anti tumor, Anti inflammatory, Anti hyperglycemia, Anti fungal, Anticonvulsant activity.

APA, Harvard, Vancouver, ISO, and other styles

41

Medvetz, Doug A., Khadijah M. Hindi, Matthew J. Panzner, Andrew J. Ditto, Yang H. Yun, and Wiley J. Youngs. "Anticancer Activity of Ag(I) N-Heterocyclic Carbene Complexes Derived from 4,5-Dichloro-1H-Imidazole." Metal-Based Drugs 2008 (July 1, 2008): 1–7. http://dx.doi.org/10.1155/2008/384010.

Full text

Abstract:

A class of Ag(I) N-heterocyclic carbene silver complexes, 1–3, derived from 4,5-dichloro-1H-imidazole has been evaluated for their anticancer activity against the human cancer cell lines OVCAR-3 (ovarian), MB157 (breast), and Hela (cervical). Silver complexes 1–3 are active against the ovarian and breast cancer cell lines. A preliminary in vivo study shows 1 to be active against ovarian cancer in mice. The results obtained in these studies warrant further investigation of these compounds in vivo.

APA, Harvard, Vancouver, ISO, and other styles

42

Harlepp, Sébastien, Edith Chardon, Mathilde Bouché, Georges Dahm, Mounir Maaloum, and Stéphane Bellemin-Laponnaz. "N-Heterocyclic Carbene-Platinum Complexes Featuring an Anthracenyl Moiety: Anti-Cancer Activity and DNA Interaction." International Journal of Molecular Sciences 20, no. 17 (August 27, 2019): 4198. http://dx.doi.org/10.3390/ijms20174198.

Full text

Abstract:

A platinum (II) complex stabilized by a pyridine and an N-heterocyclic carbene ligand featuring an anthracenyl moiety was prepared. The compound was fully characterized and its molecular structure was determined by single-crystal X-ray diffraction. The compound demonstrated high in vitro antiproliferative activities against cancer cell lines with IC50 ranging from 10 to 80 nM. The presence of the anthracenyl moiety on the N-heterocyclic carbene (NHC) Pt complex was used as a luminescent tag to probe the metal interaction with the nucleobases of the DNA through a pyridine-nucleobase ligand exchange. Such interaction of the platinum complex with DNA was corroborated by optical tweezers techniques and liquid phase atomic force microscopy (AFM). The results revealed a two-state interaction between the platinum complex and the DNA strands. This two-state behavior was quantified from the different experiments due to contour length variations. At 24 h incubation, the stretching curves revealed multiple structural breakages, and AFM imaging revealed a highly compact and dense structure of platinum complexes bridging the DNA strands.

APA, Harvard, Vancouver, ISO, and other styles

43

Nada, Hossam, Ahmed Elkamhawy, and Kyeong Lee. "Structure Activity Relationship of Key Heterocyclic Anti-Angiogenic Leads of Promising Potential in the Fight against Cancer." Molecules 26, no. 3 (January 21, 2021): 553. http://dx.doi.org/10.3390/molecules26030553.

Full text

Abstract:

Pathological angiogenesis is a hallmark of cancer; accordingly, a number of anticancer FDA-approved drugs act by inhibiting angiogenesis via different mechanisms. However, the development process of the most potent anti-angiogenics has met various hurdles including redundancy, multiplicity, and development of compensatory mechanisms by which blood vessels are remodeled. Moreover, identification of broad-spectrum anti-angiogenesis targets is proved to be required to enhance the efficacy of the anti-angiogenesis drugs. In this perspective, a proper understanding of the structure activity relationship (SAR) of the recent anti-angiogenics is required. Various anti-angiogenic classes have been developed over the years; among them, the heterocyclic organic compounds come to the fore as the most promising, with several drugs approved by the FDA. In this review, we discuss the structure–activity relationship of some promising potent heterocyclic anti-angiogenic leads. For each lead, a molecular modelling was also carried out in order to correlate its SAR and specificity to the active site. Furthermore, an in silico pharmacokinetics study for some representative leads was presented. Summarizing, new insights for further improvement for each lead have been reviewed.

APA, Harvard, Vancouver, ISO, and other styles

44

da Silveira Pinto, Ligia S., Thatyana R. Alves Vasconcelos, Claudia Regina B. Gomes, and Marcus Vinícius N. de Souza. "A Brief Review on the Development of Novel Potentially Active Azetidin-2-ones Against Cancer." Current Organic Chemistry 24, no. 5 (May 17, 2020): 473–86. http://dx.doi.org/10.2174/1385272824666200303115444.

Full text

Abstract:

Azetidin-2-ones (β-lactams) and its derivatives are an important group of heterocyclic compounds that exhibit a wide range of pharmacological properties such as antibacterial, anticancer, anti-diabetic, anti-inflammatory and anticonvulsant. Efforts have been made over the years to develop novel congeners with superior biological activities and minimal potential for undesirable side effects. The present review aimed to highlight some recent discoveries (2013-2019) on the development of novel azetidin-2-one-based compounds as potential anticancer agents.

APA, Harvard, Vancouver, ISO, and other styles

45

Li, Wu-Wu, Min-Yan Zheng, Ying Guo, Zun-Ting Zhang, Ji-Chang Han, Yan-Ping Jiang, Qiao Wang, Mei Wang, Ming-Xiang Ji, and Yu-Tao Zhang. "Construction of C-glycosides of heterocycles containing the pyrimidin-2-amine or the 1H-pyrazolo[3,4-b]pyridine moiety and their biological evaluation for anticancer activities." Journal of Chemical Research 43, no. 3-4 (March 2019): 152–57. http://dx.doi.org/10.1177/1747519819856942.

Full text

Abstract:

A series of novel C-glycosides of heterocyclic derivatives containing a pyrimidin-2-amine or a 1 H-pyrazolo[3,4- b]pyridine moiety were synthesized using condensation reactions of the substituted puerarin with guanidine or 3-amino-5-hydroxypyrazole in methyl alcohol. Their chemical structures were characterized by Fourier-transform infrared spectroscopy, nuclear magnetic resonance, and high-resolution mass spectrometry. In addition, their biological activity has been demonstrated by in vitro evaluation against the human leukemia cells K562 and human prostate cancer cells PC-3 by MTT-based assays, using the commercially available standard drug of cis-platin as a positive control. The results also demonstrated that most of the compounds showed considerable cytotoxicity to these two cell lines of K562 and PC-3, and indicated that novel C-glycosides of heterocyclic derivatives may be potential leads for further biological screenings and may generate drug-like molecules.

APA, Harvard, Vancouver, ISO, and other styles

46

Liu, Chunjing, Benyi Li, and Lester Mitscher. "Synthesis of New TGX-221 Analogs." Zeitschrift für Naturforschung B 69, no. 7 (July 1, 2014): 817–22. http://dx.doi.org/10.5560/znb.2014-4081.

Full text

Abstract:

TGX-221 is a potent phosphoinositide 3-kinase (PI3K)β inhibitor that has great therapeutic potential to treat prostate cancer. Chemical modification of TGX-221 at positions 2 and 9 was made. Five new TGX-221 analogs with different heterocyclic substituents of morpholine, 1-methylpiperazine, aniline, and thiazole-2-amine at positions 2 and 9 were synthesized. Parallel synthetic methods were employed in SN2 replacement reactions at positions 2 and 9 of TGX-221.

APA, Harvard, Vancouver, ISO, and other styles

47

Montes-González, Ingrid, Ambar M. Alsina-Sánchez, Juan C. Aponte-Santini, Sara M. Delgado-Rivera, and Geraldo L. Durán-Camacho. "Perspectives of ferrocenyl chalcones: synthetic scaffolds toward biomedical and materials science applications." Pure and Applied Chemistry 91, no. 4 (April 24, 2019): 653–69. http://dx.doi.org/10.1515/pac-2018-0802.

Full text

Abstract:

Abstract Ferrocene and its derivatives constitute versatile and interesting scaffolds for the global chemical enterprise due to its multiple applications that range from biomedical to materials science. Ferrocenyl derivatives are the leading compounds in our research for the syntheses and characterization as well as their potential biological applications. Among them, our recent focus has been in ferrocenyl chalcones as a framework for further derivatization. The proposed modifications consist on the incorporation of heterocyclic moieties into the ferrocenyl chalcone core. This can be afforded either by introducing a heterocyclic aromatic moiety as a substituent or functionalizing the α-β unsaturated system. Another modification explored is the formation of ammonium or pyridinium salts to increase water solubility. Studied ferrocenyl chalcones exhibit remarkable stability, physical, and electrochemical properties. These factors have led the approaches for them to be precursors of biologically active compounds (cancer, bacteria, malaria, and neurobiological diseases). Moreover, other potential applications include molecular materials, redox-sensors, and polymers. Our goal in this mini review is to highlight the chemistry of ferrocene derivatives with particular prominence to those ferrocenyl chalcones studied in our laboratory and their applications. Moreover, we are providing a background on ferrocene, chalcones, and ferrocenyl chalcones, emphasizing the methodologies with preeminent yields.

APA, Harvard, Vancouver, ISO, and other styles

48

Wantz, May, Mathilde Bouché, Georges Dahm, Neïla Chekkat, Sylvie Fournel, and Stéphane Bellemin-Laponnaz. "N-Heterocyclic Carbene-Polyethyleneimine (PEI) Platinum Complexes Inducing Human Cancer Cell Death: Polymer Carrier Impact." International Journal of Molecular Sciences 19, no. 11 (November 5, 2018): 3472. http://dx.doi.org/10.3390/ijms19113472.

Full text

Abstract:

The high interest in N-Heterocyclic platinum carbene complexes in cancer research stems from their high cytotoxicity to human cancer cells, their stability, as well as their ease of functionalization. However, the development of these new molecules as anticancer agents still faces multiple challenges, in particular solubility in aqueous media. Here, we synthesized platinum-NHC bioconjugates that combine water-solubility and cytotoxicity by using polyethyleneimine as polymer carrier. We showed on 8 different types of cells that the activity of these conjugates is modulated by the size of the polymer and the overall density of metal ions onto polymer chains. Using HCT116 cells, the conjugates displayed an effective activity after only 45 min of exposure in vitro correlated with a quick uptake by the cells as shown by the use of various fluorescent-tagged derivatives.

APA, Harvard, Vancouver, ISO, and other styles

49

Tandon, Runjhun, Iqubal Singh, Vijay Luxami, Nitin Tandon, and Kamaldeep Paul. "Recent Advances and Developments ofin vitroEvaluation of Heterocyclic Moieties on Cancer Cell Lines." Chemical Record 19, no. 2-3 (June 26, 2018): 362–93. http://dx.doi.org/10.1002/tcr.201800024.

Full text

APA, Harvard, Vancouver, ISO, and other styles

50

Kljun, Jakob, Saša Petriček, Dušan Žigon, Rosana Hudej, Damijan Miklavčič, and Iztok Turel. "Synthesis and Characterization of Novel Ruthenium(III) Complexes with Histamine." Bioinorganic Chemistry and Applications 2010 (2010): 1–6. http://dx.doi.org/10.1155/2010/183097.

Full text

Abstract:

Novel ruthenium(III) complexes with histamine[RuCl4(dmso-S)(histamineH)]⋅O(1a) and[RuCl4(dmso-S)(histamineH)](1b) have been prepared and characterized by X-ray structure analysis. Their crystal structures are similar and show a protonated amino group on the side chain of the ligand which is not very common for a simple heterocyclic derivative such as histamine. Biological assays to test the cytotoxicity of the compound1bcombined with electroporation were performed to determine its potential for future medical applications in cancer treatment.

APA, Harvard, Vancouver, ISO, and other styles

Journal articles on the topic 'Heterocyclic chemistry; Cancer'

Create a spot-on reference in APA, MLA, Chicago, Harvard, and other styles