Academic literature on the topic 'Synthesis of chalcones'

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Journal articles on the topic "Synthesis of chalcones"

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Chen, Jie, Chen-Fu Liu, and Guo-Wu Rao. "Progress in the Synthesis, Angiogenesis Activity and Mechanism of Chalcone Derivatives." Mini-Reviews in Organic Chemistry 17, no. 7 (October 9, 2020): 814–27. http://dx.doi.org/10.2174/1570193x17666191223161941.

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Cancer is a common disease that poses a serious threat to human health. Angiogenesis is essential for the growth and metabolism of tumors, providing oxygen and nutrition for the growth of cells and tissues. However, angiogenesis of tumors depends on the stimulation of growth factors. Vascular Endothelial Growth Factor (VEGFR) is the most unique factor. Therefore, VEGF/VEGFR targeting anticancer drugs are playing an increasingly significant role in clinical trials. In addition, it has been proved that chalcone, the precursor of natural flavonoids, has potential anti-tumor activity, especially anti-angiogenesis activity. This review summarizes the reports about the anti-angiogenesis of chalcone derivatives. Based on the chalcone skeleton, it is divided into substituted chalcones and modified chalcones. The anti-angiogenesis activities of natural or synthetic chalcones, benzene ring modified or connecting bridge modified chalcones are described in this review.
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K. Saini, K. Rajendra, S. Amit Choudhary, Yogesh C. Joshi, and P. Joshi. "Solvent Free Synthesis of Chalcones and their Antibacterial Activities." E-Journal of Chemistry 2, no. 4 (2005): 224–27. http://dx.doi.org/10.1155/2005/294094.

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The solvent free synthesis of six chalcones was carried out by grinding the piperanal and the acetophenone (unsubstituted, 4-methyl, 4-methoxy, 4-bromo, 4-nitro, 3-chloro) in the presence of solid sodium hydroxide with a mortar and pestle. In general, the chalcones were obtained in high yield and high purity. Minor quantities of Ketol and Michael addition product were easily removed by recrystallization. The result indicates a correlation between the success of the solvent-free synthesis and melting point of the chalcone. Chalcone with relatively high melting points (higher than 80°C) were obtained in high yields. The two chalcones that could not be produced in good yields were having relatively low melting points. They have been screened for their antibacterial activity against Gram positive and Gram negative bacteria.
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Jasim, Hiba A., Lutfun Nahar, Mohammad A. Jasim, Sharon A. Moore, Kenneth J. Ritchie, and Satyajit D. Sarker. "Chalcones: Synthetic Chemistry Follows Where Nature Leads." Biomolecules 11, no. 8 (August 13, 2021): 1203. http://dx.doi.org/10.3390/biom11081203.

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Chalcones belong to the flavonoid class of phenolic compounds. They form one of the largest groups of bioactive natural products. The potential anticancer, anti-inflammatory, antimicrobial, antioxidant, and antiparasitic properties of naturally occurring chalcones, and their unique chemical structural features inspired the synthesis of numerous chalcone derivatives. In fact, structural features of chalcones are easy to construct from simple aromatic compounds, and it is convenient to perform structural modifications to generate functionalized chalcone derivatives. Many of these synthetic analogs were shown to possess similar bioactivities as their natural counterparts, but often with an enhanced potency and reduced toxicity. This review article aims to demonstrate how bioinspired synthesis of chalcone derivatives can potentially introduce a new chemical space for exploitation for new drug discovery, justifying the title of this article. However, the focus remains on critical appraisal of synthesized chalcones and their derivatives for their bioactivities, linking to their interactions at the biomolecular level where appropriate, and revealing their possible mechanisms of action.
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Tantawy, Mohamed A., Farid M. Sroor, Magda F. Mohamed, Mostafa E. El-Naggar, Fatma M. Saleh, Hamdi M. Hassaneen, and Ismail A. Abdelhamid. "Molecular Docking Study, Cytotoxicity, Cell Cycle Arrest and Apoptotic Induction of Novel Chalcones Incorporating Thiadiazolyl Isoquinoline in Cervical Cancer." Anti-Cancer Agents in Medicinal Chemistry 20, no. 1 (April 10, 2020): 70–83. http://dx.doi.org/10.2174/1871520619666191024121116.

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Background: Chalcones are naturally occurring compounds found in various plant species which are widely used for the traditional popular treatments. Chalcones are distinguished secondary metabolites that are reported to display diverse biological activities such as antiviral, antiplatelet, anti-inflammatory, anticancer, antibacterial and antioxidant agents. The presence of a,ß-unsaturated carbonyl group in chalcones is assumed to be responsible for their bioactivity. In addition, heterocyclic compounds having nitrogen such as isoquinolines are of considerable interest as they constitute the core structural element of many alkaloids that have enormous pharmacological activities. Objective: The objective of this study is the synthesis and biological activity of novel chalcones incorporating thiadiazolyl isoquinoline as potential anticancer candidates. Different genetic tools were used in an attempt to know the mechanism of action of this compound against breast cancer. Methods: An efficient one pot synthesis of novel chalcones incorporating thiadiazolyl isoquinoline has been developed. The cytotoxic activity of the novel synthesized compounds was performed against four different kinds of cancer cell lines. Results: Among all the tested derivatives, chalcone 3 has the best cytotoxic profile against A549, MCF7, and HeLa cell lines, with IC50s (66.1, 51.3, and 85.1μM, respectively). Molecular docking studies for chalcone 3 revealed that CDK2, and EGFRTK domains have strong binding affinities toward the novel chalcone 3, while tubulin-colchicine-ustiloxin, and VEGFRTK domains illustrated moderate mode of binding. Conclusion: We have developed an efficient method for the synthesis of novel chalcones incorporating thiadiazolyl isoquinoline. All compounds showed better cytotoxicity results against four kinds of cancer cell lines (A549, MCF7, HCT116, and HELA cells). The results depicted that chalcone 3 has a high and promising cytotoxic effect against HELA cell line and the mechanism of cytotoxicity was widely studied through different theoretical and experimental tools. Thus, the newly synthesized derivative 3 can be utilized as a novel chemotherapeutic compound for cervical carcinoma.
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Farooq, Saba, and Zainab Ngaini. "Recent Synthetic Methodologies for Chalcone Synthesis (2013-2018)." Current Organocatalysis 6, no. 3 (September 5, 2019): 184–92. http://dx.doi.org/10.2174/2213337206666190306155140.

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An up-to-date short review of the chalcone methodologies is presented, which is the most interesting and beneficial for choosing the desired protocol to synthesize suitable derivatives of chalcones. Chalcones are fluorescent, stable compounds which contribute to the synthesis of various pharmacologically important heterocyclic structure-based derivatives. Chalcone has displayed a remarkable curative efficiency to cure several diseases. Several schemes and methodologies have been reported for employing different catalysts and reagents. The development of improved methodologies of α, β-unsaturated carbonyl compounds is still on going. In this review, synthetic methodologies and their recent modification in designing new methods with efficient, economical, eco-friendly and high yield are discussed.
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López, Génesis, Marco Mellado, Enrique Werner, Bastián Said, Patricio Godoy, Nelson Caro, Ximena Besoain, Iván Montenegro, and Alejandro Madrid. "Sonochemical Synthesis of 2’-Hydroxy-Chalcone Derivatives with Potential Anti-Oomycete Activity." Antibiotics 9, no. 9 (September 4, 2020): 576. http://dx.doi.org/10.3390/antibiotics9090576.

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This work reports on the synthesis of eight new 2′-hydroxy-chalcones with potential anti-phytopathogenic applications in agroindustry, AMONG others, via Claisen–Schmidt condensation and ultrasound assisted reaction. Assays showed three chalcones with allyl moieties strongly inhibited growth of phytopathogenic oomycete Phytophthora infestans; moreover, compound 8a had a half maximal effective concentration (EC50) value (32.5 µg/mL) similar to that of metalaxyl (28.6 µg/mL). A software-aided quantitative structure–activity relationship (QSAR) analysis of the whole series suggests that the structural features of these new chalcones—namely, the fluoride, hydroxyl, and amine groups over the carbon 3′ of the chalcone skeleton—increase anti-oomycete activity.
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Wijayanti, Lucia Wiwid, Respati Tri Swasono, Wonkoo Lee, and Jumina Jumina. "Synthesis and Evaluation of Chalcone Derivatives as Novel Sunscreen Agent." Molecules 26, no. 9 (May 4, 2021): 2698. http://dx.doi.org/10.3390/molecules26092698.

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Ultraviolet (UV) irradiation is a serious problem for skin health thus the interest in the research to develop sunscreen agent has been increasing. Chalcone is a promising compound to be developed as its chromophore absorbs in the UV region. Therefore, in the present work, we synthesized eight chalcone derivatives through Claisen–Schmidt condensation at room temperature. The evaluation of the optical properties of each chalcone derivatives in the UV region was conducted through spectroscopic and computational studies. The synthesized chalcones were obtained in good yields and they were active in the UV region. The results revealed that more methoxy substituents to chalcone leads toward red shift. All chalcone derivatives have high molar absorptivity value (21,000–56,000) demonstrating that they have the potential to be used as the sunscreen agent. The cytotoxicity assay showed that chalcone derivatives were demonstrating low toxicity toward normal human fibroblast cell, which is remarkable. Therefore, we concluded that the synthesized chalcones in this work were potential to be developed as novel sunscreen agents in real application.
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Ouyang, Yang, Juanjuan Li, Xinyue Chen, Xiaoyu Fu, Si Sun, and Qi Wu. "Chalcone Derivatives: Role in Anticancer Therapy." Biomolecules 11, no. 6 (June 16, 2021): 894. http://dx.doi.org/10.3390/biom11060894.

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Chalcones (1,3-diaryl-2-propen-1-ones) are precursors for flavonoids and isoflavonoids, which are common simple chemical scaffolds found in many naturally occurring compounds. Many chalcone derivatives were also prepared due to their convenient synthesis. Chalcones as weandhetic analogues have attracted much interest due to their broad biological activities with clinical potentials against various diseases, particularly for antitumor activity. The chalcone family has demonstrated potential in vitro and in vivo activity against cancers via multiple mechanisms, including cell cycle disruption, autophagy regulation, apoptosis induction, and immunomodulatory and inflammatory mediators. It represents a promising strategy to develop chalcones as novel anticancer agents. In addition, the combination of chalcones and other therapies is expected to be an effective way to improve anticancer therapeutic efficacy. However, despite the encouraging results for their response to cancers observed in clinical studies, a full description of toxicity is required for their clinical use as safe drugs for the treatment of cancer. In this review, we will summarize the recent advances of the chalcone family as potential anticancer agents and the mechanisms of action. Besides, future applications and scope of the chalcone family toward the treatment and prevention of cancer are brought out.
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B, Ravindar, Srinivasa Murthy M, and Afzal Basha Shaik. "DESIGN, FACILE SYNTHESIS, AND BIOLOGICAL EVALUATION OF NOVEL 1,3-THIAZINE DERIVATIVES AS POTENTIAL ANTICONVULSANT AGENTS." Asian Journal of Pharmaceutical and Clinical Research 9, no. 5 (September 1, 2016): 272. http://dx.doi.org/10.22159/ajpcr.2016.v9i5.13676.

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ABSTRACTObjective: Chalcones and their heterocyclic analogs represent an important class of small molecules having anticonvulsant activities. Therefore, inthis study, the synthesis and anticonvulsant activity of some new chalcones and 1,3-thiazines were described.Methods: The reaction of 1-acetylnaphthalene with substituted aromatic aldehydes in the presence of aq. NaOH afforded corresponding chalconeswhich upon further cyclization with thiourea resulted in 1,3-thiazine derivatives. The newly synthesized compounds were tested for anticonvulsantactivity by pentylenetetrazole-induced seizures method using diazepam as standard.Results: Most of the compounds showed good anticonvulsant activity but is less than diazepam. 1,3-thiazines were more potent than chalconesand among them, compound P4 containing 4-fluorophenyl substituents on the thiazine moiety was more potent as it has prolonged the onset ofconvulsions by 155.2 seconds.Conclusion: We described the synthesis and anticonvulsant activity of novel chalcones and 1,3-thiazine derivatives. 1,3-thiazines are more activeanticonvulsant agents than chalcones and in particular compounds with electron withdrawing substituents.Keywords: Chalcone, 1,3-thiazine, Pentylenetetrazole.
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Coşkun, Demet, Suat Tekin, Süleyman Sandal, and Mehmet Fatih Coşkun. "Synthesis, Characterization, and Anticancer Activity of New Benzofuran Substituted Chalcones." Journal of Chemistry 2016 (2016): 1–8. http://dx.doi.org/10.1155/2016/7678486.

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Benzofuran derivatives are of great interest in medicinal chemistry and have drawn considerable attention due to their diverse pharmacological profiles including anticancer activity. Similarly, chalcones, which are common substructures of numerous natural products belonging to the flavonoid class, feature strong anticancer properties. A novel series of chalcones, 3-aryl-1-(5-bromo-1-benzofuran-2-yl)-2-propanones propenones (3a–f), were designed, synthesized, and characterized.In vitroantitumor activities of the newly synthesized (3a–f) and previously synthesized (3g–j) chalcone compounds were determined by using human breast (MCF-7) and prostate (PC-3) cancer cell lines. Antitumor properties of all compounds were determined by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Cell viability assay for the tested chalcone compounds was performed and thelog⁡IC50values of the compounds were calculated after 24-hour treatment. Our results indicate that the tested chalcone compounds show antitumor activity against MCF-7 and PC-3 cell lines (p<0.05).
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Dissertations / Theses on the topic "Synthesis of chalcones"

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Baugaard, Carlo. "The synthesis and electrochemical studies of chalcones and flavanones: an investigation of their antioxidant activity." Thesis, University of Western Cape, 2013. http://hdl.handle.net/11394/3312.

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>Magister Scientiae - MSc
Flavonoids, one of the biggest classes of secondary metabolites, are found abundantly in nature in a broad range of fruits, vegetables and beverages such as tea, coffee, beer, wine and fruit drinks. Flavonoids have been reported to exert multiple biological functions as well as tremendous pharmacological activity, including anticancer activity, protection, antioxidant activity, cardiovascular protection, antibacterial, antifungal and antiviral activity. The antioxidant activity of flavones is reported to be associated with those bearing hydroxyl functions. In the present study, several reaction steps have been carried out to synthesize three sub classes of flavonoids namely; chalcones, dihydrochalcones and flavanones with various substituents attached. The first step involved protection of hydroxyl groups of acetophenone and benaldehyde as starting materials. Thereafter the Clasien Schmidt condensation reaction, under basic conditions, was performed to afford chalcone intermediates. Treatment of these chalcones with sodium acetate, under reflux, afforded flavanones as a single product in high yields. Thereafter all protecting groups where removed to yield the final products. All products and intermediates where purified by column chromatography and were characterized by Nuclear Magnetic Resonance Spectroscopy (NMR) (1H NMR and 13C NMR). An electrochemical analysis on all flavonoid compounds was performed by Cyclic Voltammetry (CV) and Square Wave Voltammetry (SWV) to give information on the accessible redox couples identified by their oxidation potentials. Oxidation potentials, which gave valuable information about reducing ability and hence the antioxidant activity, where used to compare all compounds. The antioxidant activity was observed to increase with the addition of hydroxyl groups on the B-ring. Compounds with a combination of hydroxyl groups on the A-ring and methoxy groups on the B-ring showed increased antioxidant activity when compared to those with only hydroxyl groups on the base structure. 2, 5, 4’-trihydroxy dihydrochalcone showed moderate antioxidant ability. However the 2, 5, 4’-trihydroxychalcone, containing the α, β unsaturated double bond, proved to have the greatest antioxidant ability.
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Armitage, Edward Simon Marco. "Design and synthesis of Combretastatin A-4 like chalcones and their analogues, and other anticancer agents." Thesis, Cardiff University, 2007. http://orca.cf.ac.uk/56191/.

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This thesis covers work investigating the design, synthesis and evaluation of Combretastatin A-4 like chalcones and their analogues, and other anticancer agents. The first two chapters are an introduction to cancer chemotherapy and the development of tubulin as a target for chemotherapy. Chapter one includes information on cancer epidemiology, the history of cancer and the development of important cancer chemotherapy agents. While the second chapter describes the role of tubulin in mitosis, and the development of anticancer agents that target tubulin. The third chapter describes the background to the chalcone project, as well as the design and synthesis of new Combretastatin A-4 like chalcones and their analogues. To further the investigation of the substitution of the a-hydrogen of the chalcone with various groups, a series of a-arylchalcones was synthesized. The substitution of a-hydrogen with various aryl groups generally shows a significant increase in the anticancer activity of the chalcone. The effect of the conformation of the chalcone on its anticancer activity was also investigated by synthesizing two series of chalcone analogues which mimic the s-trans arrangement of chalcone, the indanones and indenones. Several of the indanones and indenones showed high levels of cytotoxicity with the CA-4 like indenone having an IC5o(K562) value of 0.019 uM. Chapter four looks at other chalcones with anticancer activity including the naturally occurring chalcone 4-hydroxyderricin, which has been isolated from the roots of Angelica keiskei and has shown to have anti-tumour promoting properties. As part of my PhD study the natural product 4-hydroxyderricin and a series of analogues was synthesized to investigate its anticancer activity. In chapter five I synthesized the anticancer agent KNK437 which has been shown to be a dose dependant inhibitor of the acquisition of thermotolerance in several different tumours. The study found that KNK437 sensitizes human leukaemia cells to the 17-allylamino-demethoxy geldanamycin induced apoptosis.
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Anjos, Murilo Machado dos. "Síntese, otimização e avaliação da atividade biológica de derivados de chalconas." Universidade Federal de Goiás, 2015. http://repositorio.bc.ufg.br/tede/handle/tede/5610.

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Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPES
The world's population sees aging and some diseases that become more common. Alzheimer's disease (AD) is a dementia caused by loss of cognitive function of the individual and drugs used in their treatment is based on the inhibition of the enzyme acetylcholinesterase (AChE). Cancer is a group of diseases that develop due to the disorderly proliferation of cells may be related to genetic factors as well as dietary habits and exposure to radiation, the treatment being based on three main techniques: surgery, radiation and chemotherapy. In this work we synthesized 15 compounds (11 chalcones and 4 imines), based on the condensation of Claisen-Smth, and they are characterized by NMR (1H and 13C), IV These compounds were submitted to acetylcholinesterase activity by the modified method of Elman, using CCD and Martson, in addition to the evaluation of cytotoxic tumorias lines SF-295 (glioblastoma - human), HL-60 (acute leukemia promielítica) and HCT-116 (colon). The compounds showed no activity for the enzyme AChE front of the methods employed, and this cause investigated using molecular modeling methods, which sought in the literature active compounds for this enzyme, containing resemblance with the structures synthesized in this work. 80 descriptors were calculated being submitted to statistical analysis (Fisher's weight) where the number of variables is reduced to 24 and these have been selected GAP and bond angle where it was observed that the values of the synthesized compounds, mostly It was found out of range for the active compounds. The previous modeling studies are not sufficient to determine the causes of inactivity of the compounds, being necessary to the realization of a structure and reactivity studies. The evaluation of the antitumor compounds presented become more positive as the MCH-1
A população mundial veem envelhecendo e com isto algumas doenças tornam-se mais comum. A doença de Alzheimer (DA) é uma demencia causada pela perda da função cognitiva do indivíduo e as drogas empregadas no seu tratamento tem como base a inibição da enzima acetilcolinesteráse (AChE). O cancer é um conjunto de doenças que se desenvolvem pela multiplicação desordenada de células, pode estar relacionado com fatores genéticos como também hábitos alimentares e exposição à radiação, sendo o tratamento baseado em três principais técnicas: cirurgia, radioterapia e quimioterapia. Neste trabalho foram sintetizados 15 compostos (11 chalconas e 4 iminas), baseando-se na condensação de Claisen-Smth, sendo os mesmos caracterizados por RMN (1H e 13C) e I.V. Estes compostos foram submetidos à atividade anticolinesterásica pelo método modificado de Elman, utilizando-se CCD, e Martson, além da avaliação citotóxica para as linhagens tumorias SF-295 (glioblastoma - humano), HL-60 (leucemia promielítica aguda) e HCT-116 (colón). Os compostos não apresentaram atividade para a enzima AChE frente aos métodos empregado, sendo esta causa investigada utilizando métodos de modelagem molecular, onde buscou-se na literatura compostos ativos para esta enzima, que continham similiaridades com as estruturas sintetizadas neste trabalho. Foram calculados 80 descritores sendo estes submetidos à uma análise estátistica (peso de fisher) onde o número de variáveis foi reduzido para 24 e destas foram selecionadas o GAP e ângulo de ligação, onde observou-se que os valores dos compostos sintetizados, em sua maioria, estavam fora da faixa encontrada para os compostos ativos. Os estudos prévios de modelagem não são suficientes para determinar as causas da inatividade dos compostos, sendo necessário a realização de um estudo de estrutura e reatividade. A avaliação antitumoral dos compostos apresentou-se mais positiva, sendo as chalconas Mch-1 e Mch-7 ativas para duas linhagens celulares tumorais (HCT-116 e SF-265).
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Rivera, Sylvie. "Synthèse et réactivité des chalcones." Paris 5, 1997. http://www.theses.fr/1997PA05P150.

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Schicker, Susanna Heidi. "Synthesis of intermediates for chalcone and 6-MSA biosynthesis." Thesis, University of Bristol, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.336910.

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Zakai, Uzma I. "Design, Synthesis, and Evaluation of Chalcogen Interactions." Diss., The University of Arizona, 2007. http://hdl.handle.net/10150/195272.

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Contributions in the area of cationic chalcogen-chalcogen and chalcogen-π interactions as well as chalcogen mediated Group 14-iron interactions have been made. This work reports the electrochemical oxidation of 8- and 10-membered ring dichalcogenides appended with β-silicon and tin substituents. The heterocycles with tellurium undergo reversible oxidation but those with sulfur or selenium are irreversibly oxidized. The ionization energies of these mesocyclic chalcogenoethers were determined by photoelectron spectroscopy. These lowest ionization energies reflect substantial (0.53-0.75 eV) orbital destabilizations due to the neighboring C-Si or C-Sn bonds. In particular, a novel Si-Si effect on the ionization of these β-disilyl sulfides and selenides was found by PES measurements. Fe₂S₂(CO)₆ clusters with a C-Sn or C-Sn-C moiety bridging the sulfur atoms or a CH₂SnMe₃ group attached to each sulfur have also been studied by photoelectron spectroscopy. Stannylation lowers the ionization energy of sulfur lone pair orbitals in these systems owing to a geometry dependent interaction as well as the Fe-Fe HOMO. Additionally, various sulfur and phosphine substituted hydroquinone and catechol redox ligands have been synthesized to append to iron sulfur clusters. Lastly, model m-terphenyl methyl and phenyl chalcogenoethers that will be further used to study cationic aromatic-chalcogen interactions have been synthesized in either of two ways. Suzuki couplings of 2,6-dibromoaniline and (2,6-diiodo-4-methylphenyl)(methyl)sulfane afford m-terphenyl methyl thioethers in 27-42% yield. Deprotonation of 1,3-dichlorobenzene and treatment with substituted aryl Grignard reagents generated m-terphenyl anions which were quenched with alkyl or aryl dichalcogenides to give m-terphenyl chalcogenoethers in 16-74% yields. A new synthesis of phenyl m-terphenyl chalcogenoethers was found. Treatment of substituted iodo-m-terphenyls with diphenyl dichalcogenides using CsOH⋅H₂O in DMSO affords phenyl m-terphenyl chalcogenoethers in 19-84% yields. Extending the scope of this methodology to other 2,6-blocked aryl halides as well as the use of aliphatic and aromatic thiols or secondary alicyclic amines has been initially explored. Finally, o-methoxy substituted m-terphenyl chalcogenoethers show atropisomerism, with barriers in the range of 66-80 kJ/mol, as determined by variable temperature ¹H NMR spectroscopic studies.
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Malmström, Jonas. "Synthesis, properties and applications of chalcogen-containing antioxidants." Doctoral thesis, Uppsala University, Department of Chemistry, 2000. http://urn.kb.se/resolve?urn=urn:nbn:se:uu:diva-1085.

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In the first part, the preparation and properties of chalcogen-containing vitamin E analogues are described. The sulfur compound 3,3,4,6,7-pentamethyl-2,3-dihydrobenzo[b]thiophene-5-ol was prepared by two different routes using ionic and radical chemistry. Interesting rearrangements were observed in the two synthetic pathways.

A new methodology for the synthesis of dihydroselenophene and dihydrotellurophene derivatives is described. In the preparation of the vitamin E analogues 2,3-dihydrobenzo[b]selenophene-5-ol and 2,3-dihydrobenzo[b]tellurophene-5-ol a tellurium-mediated tandem SRN1/SHi sequence was suggested to be operative. 2,3-Dihydrobenzo[b]thiophene-5-ol and the vitamin E-like selenide 2-methyl-2-(4,8,12-trimethyl-tridecyl)-selenochroman-6-ol were prepared via intramolecular homolytic substitution at sulfur and selenium, respectively. The first rate constant for intramolecular homolytic substitution at tellurium is also reported (5x108 s-1 at 25 °C).

The antioxidant profile for 2,3-dihydrobenzo[b]furan-5-ol and its 1-thio, 1-seleno, and 1-telluro analogues is described. By means of pulse radiolysis, it was shown that the one-electron reduction potentials (ArO·/ArO-) were independent of the chalcogen (0.49-0.52 V vs NHE). The O-H bond dissociation enthalpies for the compounds were also estimated to be similar (336-340 kJ mol-1). The pKa values and the oxidation potentials were also determined for these compounds. For some compounds the rate of hydrogen atom donation to tert-butoxyl radicals was determined by means of laser flash photolysis. Using a two-phase lipid peroxidation model, it was demonstrated that the selenium and tellurium analogues could be regenerated in the presence of a stoichiometric amount of a reducing agent. The organotellurium analogue also acted as a good glutathione-peroxidase mimic and as a potent inhibitor of lipid peroxidation in liver microsomes.

In the second part of the thesis the stabilizing capacity of bis[4-(dimethylamino)phenyl]telluride was investigated in the thermoplastic elastomer PACREL®. It was demonstrated that the addition of 0.17-0.50 % of the telluride significantly improved the tensile strength and elongation at break of the polymer. Chemiluminescence measurements showed that the organotellurium compound prolonged the induction period of thermo-oxidation and reduced the total luminescence intensity of the material.

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Evangelista, Fernanda Cristina Gontijo. "Evaluation of in vitro antitumor activity of triazole / azide synthetic chalcones." Instituto Nacional de Pesquisas da Amazônia, 2018. http://bdtd.inpa.gov.br/handle/tede/2639.

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Made available in DSpace on 2018-10-22T15:15:33Z (GMT). No. of bitstreams: 2 Avaliação de atividade antitumoral in vitroELIDA.PDF: 334912 bytes, checksum: 7e3630670b1d8ca55012362260918128 (MD5) license_rdf: 0 bytes, checksum: d41d8cd98f00b204e9800998ecf8427e (MD5) Previous issue date: 2018-10-01
Fundação de Amparo à Pesquisa do Estado de São Paulo - FAPESP
Many compounds isolated from lichens exhibit biological activity, and a number of them are proven sources of antitumor drugs. Even simple structural changes to these bioactive compounds can lead to potentiation of their activity. The purposes of this study were to evaluate the antiproliferative activity and selectivity of the following compounds isolated from lichens: atranorin; diffractaic, divaricatic, perlatolic, psoromic, norstitic, protocetraric, and fumarprotocetraric acids; and alkyl derivatives. Cytotoxicity tests based on the sulforhodamine B dye were performed on seven lines of neoplastic cells and one line of normal cells (3T3)
Muitas substâncias isoladas de liquens apresentam atividades biológicas, e algumas demonstraram ser fontes promissoras de drogas antitumorais. Modificações estruturais simples a partir dessas substâncias bioativas podem levar a potencialização da atividade apresentada. Os objetivos deste estudo foram avaliar a atividade antiproliferativa e seletividade dos seguintes compostos isolados de liquens: atranorina, ácidos difractaico, divaricático, perlatólico, psorômico, norstítico, protocetrárico e fumarprotocetrárico e derivados alquílicos. O ensaio de citotoxicidade foi realizado com corante sulforrodamina B em sete linhagens de células neoplásicas e uma linhagem de células normais (3T3)
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鄭重展 and Chung-chin Cheng. "Syntheses and photophysics of luminescent polynuclear coinage metal complexes with chalcogen and pnictogen: containing bridging ligands." Thesis, The University of Hong Kong (Pokfulam, Hong Kong), 2001. http://hub.hku.hk/bib/B31241530.

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Khan, Jamal Rafique. "Synthesis of heterocycles containing chalcogens by C-H functionalization." reponame:Repositório Institucional da UFSC, 2014. https://repositorio.ufsc.br/xmlui/handle/123456789/131002.

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Tese (doutorado) - Universidade Federal de Santa Catarina, Centro de Ciências Físicas e Matemáticas, Programa de Pós-Graduação em Química, Florianópolis, 2014.
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No presente trabalho desenvolveram-se novas metodologias eficientes, econômicas e ambientalmente adequadas para a síntese de oxadiazóis e benzotiazóis contendo uma porção organocalcogênio. Primeiramente, desenvolvemos a síntese de oxadiazóis selenados e tiolados através da funcionalização de ligação Csp2-H promovida por K2CO3, em um meio reacional livre de metais de transição. Em uma primeira etapa foram preparados oxadiazóis selenados com potencial para aplicações biológicas. Sob condições suaves, a reação ocorreu de maneira eficiente na presença de um equivalente do correspondente oxadiazol I, um equivalente de base (K2CO3), 0,5 equivalentes do correspondente dicalcogeneto de organoíla II, na presença de ar atmosférico. Através dessa metodologia, uma série de oxadiazóis calcogenados III na posição 5 do heterociclo foram obtidos em rendimentos que variaram de bons a excelentes. Adicionalmente, explorou-se a reatividade dos oxadiazóis selenados 3 em reações de troca calcogênio-lítio. Os intermediários oxadiazóis litiado assim obtidos foram capturados, in situ, com diferentes eletrófilos. É importante salientar, também que essa reação ocorreu de forma eficiente quando se aumentou sua escala para 10 mmol.Em uma segunda etapa desenvolvemos um novo método para a incorporação de calcogênios em benzotiazóis via reação de calcogenação direta da ligação C-H. Realizou-se a síntese de 2-organocalcogeno-1,3- benzotiazóis V através da calcogenação direta entre 1,3-benzotiazóis IV e dicalcogenetos de organoíla II catalizada por Fe3O4 nanopartículado. Esta metodologia permitiu a obtenção dos respectivos produtos calcogenolados V, em rendimentos que variaram de moderados a excelentes. Realizou-se, também, com sucesso, a reciclagem do catalisador em 4 ciclos sem um decréscimo acentuado no rendimento.

Abstract : In the present work, we developed efficient, economical and greener procedures for to the synthesis of chalcogenated oxadiazoles and benzothiazoles. In the first part, we developed a K2CO3-promoted procedure for the synthesis of selenated and thiolated oxadiazoles 3 through Csp2-H bond functionalization, under transition metal-free conditions. We prepared for the first time selenated oxadiazoles, compounds with potential for biological applications. Under mild conditions, the reaction worked well in the presence of 1equiv. of oxadiazole I, a half equiv. of diorganyl dichalcogenides II, 1 equiv. of base (K2CO3), without the exclusion of air and moisture, affording a wide range of chalcogenated oxadiazoles III at the C5 position in good to excellent yields. The various substituents with different electronic effects and steric effects tolerated the optimized reaction conditions. Furthermore, selenated oxadiazole was explored for selenium-lithium exchange reaction and lithium-intermediate was trapped by different electrophiles. We were also successful in scaling up the reaction in up to 10 mmol. Subsequently, we developed a new method of incorporation of organoyl chalcogenides in benzothiazoles via direct chalcogenation of C-H bond. In this work, we report the synthesis of 2-organochalcogeno-1,3-benzothiazoles V via direct chalcogenation reactions between 1,3-benzothiazoles IV and diorganyl dichalcogenides II catalyzed by Fe3O4 nano particle. This methodology allowed us to obtain 2-chalcogen-1,3-benzothiazoles in moderate to excellent yields, as well as recycling successful the catalyst in up to 4 cycles without any major decrease in the yield.
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Books on the topic "Synthesis of chalcones"

1

Mal, Joyabrata. Microbial Synthesis of Chalcogenide Nanoparticles: Combining Bioremediation and Biorecovery of Chalcogen in the Form of Chalcogenide Nanoparticles. Taylor & Francis Group, 2018.

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Mal, Joyabrata. Microbial Synthesis of Chalcogenide Nanoparticles: Combining Bioremediation and Biorecovery of Chalcogen in the Form of Chalcogenide Nanoparticles. Taylor & Francis Group, 2018.

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Mal, Joyabrata. Microbial Synthesis of Chalcogenide Nanoparticles: Combining Bioremediation and Biorecovery of Chalcogen in the Form of Chalcogenide Nanoparticles. Taylor & Francis Group, 2018.

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Mal, Joyabrata. Microbial Synthesis of Chalcogenide Nanoparticles: Combining Bioremediation and Biorecovery of Chalcogen in the Form of Chalcogenide Nanoparticles. Taylor & Francis Group, 2018.

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Gates, Derek Patrick. The synthesis, structures, reactivity and polymerization behavior of boron- and sufur-nitrogen-phosphorus heterocycles and highly strained chalcogen- and boron-bridged [1]ferrocenophanes. Dept of Chemistry, U of Toronto, 1997.

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Book chapters on the topic "Synthesis of chalcones"

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Misra, Ram A. "Reactivity of Superoxide Ion with Organohalogens and Chalcones." In Novel Trends in Electroorganic Synthesis, 275–77. Tokyo: Springer Japan, 1998. http://dx.doi.org/10.1007/978-4-431-65924-2_83.

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Masesane, Ishmael B., and Ofentse Mazimba. "NaBH4-Mediated Complete Reduction of the α,β-Unsaturated Ketone Units of Chalcones in the Synthesis of Flavans." In Chemistry: The Key to our Sustainable Future, 229–35. Dordrecht: Springer Netherlands, 2013. http://dx.doi.org/10.1007/978-94-007-7389-9_16.

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Begum, Shaheen, S. K. Arifa Begum, A. Mallika, and K. Bharathi. "Synthesis, Evaluation and in Silico Studies of 4-N, N-Dimethylamino and 4-Carboxy Chalcones as Promising Antinociceptive Agents." In Learning and Analytics in Intelligent Systems, 481–90. Cham: Springer International Publishing, 2020. http://dx.doi.org/10.1007/978-3-030-46939-9_42.

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Manchanayakage, Renuka. "One-Pot Synthesis of Chalcone Epoxides via Claisen Schmidt Condensation and Epoxidation." In ACS Symposium Series, 111–22. Washington, DC: American Chemical Society, 2016. http://dx.doi.org/10.1021/bk-2016-1233.ch007.

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Nogami, T., H. Nakano, S. Ikegawa, K. Miyawaki, Y. Shirota, S. Harada, and N. Kasai. "Synthesis and Crystal Structures of Multi-Chalcogen TTF Derivatives and Conducting Organic Salts." In Springer Proceedings in Physics, 373–78. Berlin, Heidelberg: Springer Berlin Heidelberg, 1990. http://dx.doi.org/10.1007/978-3-642-75424-1_80.

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Cazarolli, Luisa Helena, Virginia Demarchi Kappel, Ana Paula Zanatta, Daniela Ota Hisayasu Suzuki, Rosendo Augusto Yunes, Ricardo José Nunes, Moacir Geraldo Pizzolatti, and Fátima Regina Mena Barreto Silva. "Natural and Synthetic Chalcones." In Studies in Natural Products Chemistry, 47–89. Elsevier, 2013. http://dx.doi.org/10.1016/b978-0-444-62615-8.00002-3.

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Collier, S. J. "Synthesis from Acylsulfenyl Halides and Chalcogen Nucleophiles." In Three Carbon-Heteroatom Bonds: Acid Halides; Carboxylic Acids and Acid Salts, 1. Georg Thieme Verlag KG, 2007. http://dx.doi.org/10.1055/sos-sd-020-01529.

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Potapov, V. A., and B. A. Trofimov. "Synthesis from Metal Acetylides and Chalcogen Electrophiles." In Three Carbon-Heteroatom Bonds: Ketenes and Derivatives, 1. Georg Thieme Verlag KG, 2006. http://dx.doi.org/10.1055/sos-sd-024-00955.

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Potapov, V. A., and B. A. Trofimov. "Synthesis from Metal Acetylides and Chalcogen Halides." In Three Carbon-Heteroatom Bonds: Ketenes and Derivatives, 1. Georg Thieme Verlag KG, 2006. http://dx.doi.org/10.1055/sos-sd-024-00967.

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Afarinkia, K., and V. Vinader. "Synthesis by Electrocyclization." In Six-Membered Hetarenes with One Chalcogen, 1. Georg Thieme Verlag KG, 2003. http://dx.doi.org/10.1055/sos-sd-014-00205.

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Conference papers on the topic "Synthesis of chalcones"

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Septianingtyas, Dewi, Nahda Zafira, Zulhipri, Fera Kurniadewi, and Hanhan Dianhar. "Green synthesis of chalcones derivatives." In THE 2ND SCIENCE AND MATHEMATICS INTERNATIONAL CONFERENCE (SMIC 2020): Transforming Research and Education of Science and Mathematics in the Digital Age. AIP Publishing, 2021. http://dx.doi.org/10.1063/5.0042002.

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Silva, Marina Goulart da, Graziele Diniz da Silva, Clebson L.Veber, Andersson Barison, Gustavo H. R. Viana, and José Augusto F. P. Villar. "Design and synthesis of triazole-chalcones." In 14th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-14bmos-r0263-1.

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Santos, *Mariana Bastos dos, Fernanda Patricia Gullo, Luiz Antonio Dutra, Maria José Soares Mendes-Giannini, Ana Marisa Fusco-Almeida, and Luis Octávio Regasini. "Preparation of New Prenylated (E)-Chalcones." In 15th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-15bmos-bmos2013_201382002510.

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Silva, Wender A., Lennine R. Melo, and Júlia Galvez B. Pedreira. "Microwave Assisted Reduction of Chalcones: A Versatile Method." In 14th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-14bmos-r0352-1.

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Deobald, Anna Maria, Arlene G. Corrêa, and Márcio W. Paixão. "Application of New Organocatalysts on Asymmetric Epoxidation of Chalcones." In 14th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-14bmos-r0188-2.

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Pessôa, Jaqueline C., Pãmella C. O. de Oliveira, Meliza J. da C. Fonseca, Sergio Pinheiro, Estela M. F. Muri, Ayres G. Dias, and Paulo R. R. Costa. "Synthesis of some 1,2,3-triazole-chalcones as potential anticancer agents." In 15th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-15bmos-bmos2013_201391311340.

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Tran, Thanh-Dao, Cat-Dong Tran, Khac-Minh Thai, Tuong-Ha Do, and Thao-Nhu Nguyen. "Synthesis and Antimicrobial Activity of Novel Heterocyclic Chalcones." In The 15th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2011. http://dx.doi.org/10.3390/ecsoc-15-00789.

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Gonda, T., B. Ötvös Sándor, and A. Hunyadi. "Synthesis of new, potentially bioactive chalcones as protoflavone analogues." In GA 2017 – Book of Abstracts. Georg Thieme Verlag KG, 2017. http://dx.doi.org/10.1055/s-0037-1608257.

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Silva, Wender A., Lennine R. Melo, Guilherme R. Oliveira, Camilla C. C. Silva, and Gustavo H. G. Trossini. "Rational Synthesis, Photophysical and Biochemical Evaluation of Fluorescents Chalcones as Inhibitors of Cruzain from Trypanosoma cruzi." In 15th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-15bmos-bmos2013_2013915192751.

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Tran, Dao, Minh Nguyen, Vi Nguyen, Dat Truong, and Ha Do. "Synthesis and cytotoxic activities of some heterocyclic chalcones ." In The 19th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2015. http://dx.doi.org/10.3390/ecsoc-19-b003.

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