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Journal articles on the topic 'MCF-7 and HCT116 cell lines'

Author: Grafiati

Published: 5 June 2025

Last updated: 2 August 2025

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1

Imieje, Vincent O., Ahmed A. Zaki, Mansour A. E. Bashar, et al. "DFT Calculations, Pro-Apoptotic Effects, and Anti-Infective Investigations of Alkaloids Isolated from the Stem Bark Extract of Enantia chlorantha." Drugs and Drug Candidates 3, no. 1 (2024): 291–310. http://dx.doi.org/10.3390/ddc3010017.

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Fractionation of the stem bark of Enantia chlorantha Oliv yields three alkaloids, palmatine (1), jatrorrhizine (2), columbamine (3), and β-Sitosterol (4). In this investigation, density functional theory (DFT) calculations were carried out to evaluate the electronic structure and properties of 1–4 by DFT-B3LYP/6-31G level of theory using Gaussian 09 software. The highest occupied molecular orbital (HOMO), lowest unoccupied molecular orbital (LUMO), HOMO-LUMO energy difference (band gap), hardness (η), softness (S), dipole moment (μ), electronegativity (χ), hydrophobicity (logP), topological su

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2

Rahman, Faiz-Ur, Amjad Ali, Rong Guo, et al. "Synthesis and anticancer activities of a novel class of mono- and di-metallic Pt(ii)(salicylaldiminato)(DMSO or Picolino)Cl complexes." Dalton Transactions 44, no. 5 (2015): 2166–75. http://dx.doi.org/10.1039/c4dt03018d.

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Mono- and di-metallic Pt(ii)(salicylaldiminato)(DMSO or Picolino)Cl complexes as potential cytotoxic agents against tested human breast (MCF-7), liver (HepG2), lung (A549), colon (HCT116) and cervical (Hela) cancer cell lines.

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3

Hamdy, Ahmed K., Mahmoud M. Sheha, Atef A. Abdel-Hafez, and Samia A. Shouman. "Design, Synthesis, and Cytotoxicity Evaluation of Novel Griseofulvin Analogues with Improved Water Solubility." International Journal of Medicinal Chemistry 2017 (December 7, 2017): 1–12. http://dx.doi.org/10.1155/2017/7386125.

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Griseofulvin 1 is an important antifungal agent that has recently received attention due to its antiproliferative activity in mammalian cancer cells. Study of SAR of some griseofulvin analogues has led to the identification of 2′-benzyloxy griseofulvin 3, a more potent analogue which retards tumor growth through inhibition of centrosomal clustering. However, similar to griseofulvin 1, compound 3 exhibited poor aqueous solubility. In order to improve the poor water solubility, six new griseofulvin analogues 5–10 were synthesized and tested for their antiproliferative activity and water solubili

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4

Abdelgawad, Mohamed A., Khaled El-Adl, Sanadelaslam S. A. El-Hddad та ін. "Design, Molecular Docking, Synthesis, Anticancer and Anti-Hyperglycemic Assessments of Thiazolidine-2,4-diones Bearing Sulfonylthiourea Moieties as Potent VEGFR-2 Inhibitors and PPARγ Agonists". Pharmaceuticals 15, № 2 (2022): 226. http://dx.doi.org/10.3390/ph15020226.

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Newly designed thiazolidine-2,4-diones 3–7a–c were synthesized, and their anticancer activities were screened against three cancer lines. They showed potent activities against HepG2 compared to the other HCT116 and MCF-7 tumor cell lines. Compounds 7c and 6c were detected as highly effective derivatives against MCF-7 (IC50 = 7.78 and 8.15 µM), HCT116 (IC50 = 5.77 and 7.11 µM) and HepG2 (IC50 = 8.82 and 8.99 µM). The highly effective derivatives 6a–c and 7a–c were tested against VERO normal cell lines. All derivatives were evaluated for their VEGFR-2 inhibitory actions and demonstrated high to

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5

Alsulaimany, Marwa, Khaled El-Adl, Ahmed K. B. Aljohani, et al. "Design, synthesis, docking, ADMET and anticancer evaluations of N-alkyl substituted iodoquinazoline derivatives as dual VEGFR-2 and EGFR inhibitors." RSC Advances 13, no. 51 (2023): 36301–21. http://dx.doi.org/10.1039/d3ra07700d.

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Fifteen new 1-alkyl-6-iodoquinazoline derivatives 5a–d to 9a–e were designed and synthesized and their anticancer activities were evaluated against HepG2, MCF-7, HCT116 and A549 cancer cell lines via dual targeting of EGFR and VEGFR-2.

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6

El Malah, Tamer, Hany F. Nour, A. A. Nayl, R. A. Elkhashab, Farouk M. E. Abdel-Megeid, and Mamdouh M. Ali. "Anticancer Evaluation of Tris(triazolyl)triazine Derivatives Generated via Click Chemistry." Australian Journal of Chemistry 69, no. 8 (2016): 905. http://dx.doi.org/10.1071/ch16006.

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Click chemistry has been utilised for the preparation of new tris(triazolyl)triazines containing aliphatic and polar side chains through coupling of 2,4,6-triethynyl-[1,3,5]triazines, which possess free terminal alkyne moieties with substituted aromatic azides. The cytotoxic activity and in vitro anticancer potential of the newly synthesised compounds have been evaluated against seven human cancer cell lines including liver HepG2, breast MCF-7, lung A549, acute myeloid leukemia HL-60, colon HCT116, and prostate PC3 cancer cell lines in addition to human normal melanocyte, HFB4. The results rev

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7

El-Masry, Omar S., Arafat Goja, Mostafa Rateb, Amani Y. Owaidah, and Khaldoon Alsamman. "RNA sequencing identified novel target genes for Adansonia digitata in breast and colon cancer cells." Science Progress 104, no. 3 (2021): 003685042110320. http://dx.doi.org/10.1177/00368504211032084.

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Adansonia digitata exhibits numerous beneficial effects. In the current study, we investigated the anti-cancer effects of four different extracts of A. digitata (polar and non-polar extracts of fruit powder and fibers) on the proliferation of human colon cancer (HCT116), human breast cancer (MCF-7), and human ovarian cancer (OVCAR-3 and OVCAR-4) cell lines. RNA sequencing revealed the influence of the effective A. digitata fraction on the gene expression profiles of responsive cells. The results indicated that only the polar extract of the A. digitata fibers exhibited anti-proliferative activi

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8

Żurawska, Katarzyna, Daria Burdalska, Magdalena Skonieczna, et al. "Glycoconjugates of Mucochloric Acid—Synthesis and Biological Activity." Pharmaceuticals 16, no. 4 (2023): 525. http://dx.doi.org/10.3390/ph16040525.

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The pharmacological effects of the presence of a sugar moiety, 1,2,3-triazole ring and silyl groups in the structure of biologically active compounds have been extensively studied in drug design and medicinal chemistry. These components can be useful tools to tailoring the bioavailability of target molecules. Herein we present the study on the impact of the sugar substituent structure and triisopropylsilyl group presence on the anticancer activity of mucochloric acid (MCA) derivatives containing the furan-2(5H)-one or 2H-pyrrol-2-one core. The obtained results clearly indicated that tested com

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9

Potapova, Olga, Myriam Gorospe, Ryan H. Dougherty, Nicholas M. Dean, William A. Gaarde, and Nikki J. Holbrook. "Inhibition of c-Jun N-Terminal Kinase 2 Expression Suppresses Growth and Induces Apoptosis of Human Tumor Cells in a p53-Dependent Manner." Molecular and Cellular Biology 20, no. 5 (2000): 1713–22. http://dx.doi.org/10.1128/mcb.20.5.1713-1722.2000.

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ABSTRACT c-Jun N-terminal kinase (JNK) plays a critical role in coordinating the cellular response to stress and has been implicated in regulating cell growth and transformation. To investigate the growth-regulatory functions of JNK1 and JNK2, we used specific antisense oligonucleotides (AS) to inhibit their expression. A survey of several human tumor cell lines revealed that JNKAS treatment markedly inhibited the growth of cells with mutant p53 status but not that of cells with normal p53 function. To further examine the influence of p53 on cell sensitivity to JNKAS treatment, we compared the

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Zheng, Ling-Li, Guan Wen, Yun-Xin Yao, Xiao-Huan Li, and Feng Gao. "Design, Synthesis, and Anticancer Activity of Natural Product Hybrids With Paclitaxel Side Chain Inducing Apoptosis in Human Colon Cancer Cells." Natural Product Communications 15, no. 4 (2020): 1934578X2091729. http://dx.doi.org/10.1177/1934578x20917298.

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Based on the strong activity dependence of paclitaxel (PTX; Taxol) or docetaxel (Taxotere) on the C-13 side chain, a small library of dehydroepiandrosterone, cholesterol, vitamin D2, and alkaloids talatisamine and songorine-PTX hybrids have been synthesized and evaluated for in vitro anticancer activity by MTT assay against human breast (MCF-7), colon (HCT116), lung carcinoma (A549), and renal adenocarcinoma (786-0) cancer cell lines. Most hybrids (11b, 12b, 13b, 15b, and 18b) reduced the growth of MCF-7 and 786-0 cells with low PTX sensitivity in vitro. Among the synthesized compounds, hybrid

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11

Lu, Chong-Yu, Hong-Xiang Li, Sha Li, et al. "Two Diarylundecanones Isolated from Ardisia tenera." Natural Product Communications 12, no. 9 (2017): 1934578X1701200. http://dx.doi.org/10.1177/1934578x1701200920.

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Ardisinones G-H (1–2), two new diarylundecanones, were isolated from the ethanol extract of aerial parts of Ardisia tenera Mez. Their structures were elucidated by interpretation of the spectroscopic evidence. The isolated compounds were evaluated for cytotoxicity against four cell lines (MV4–11, MCF-7, HCT116 and A549) and displayed moderate inhibitory activities.

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12

Badem, Merve, Sıla Ozlem Sener, Seyda Kanbolat, et al. "Evaluation of biological activities of Barbarea integrifolia and isolation of a new glucosinolate derivated compound." Zeitschrift für Naturforschung C 76, no. 9-10 (2021): 375–82. http://dx.doi.org/10.1515/znc-2020-0305.

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Abstract The aim of the present study is to determine the potent biological activities and carry out isolation studies on Barbarea integrifolia. The antioxidant capacity of the species was evaluated by total phenolic content, FRAP, CUPRAC, and DPPH radical scavenging activity. Anticancer activity studies were performed by MTT assay in MDA-MB-231, MCF-7, Hep3B, PC-3, A549, HCT116, L-929 cell lines. It was observed that the remaining aqueous fraction has higher total phenolic content while higher activity in the CUPRAC and FRAP assays was displayed for the methanolic extract and chloroform fract

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13

Hussein, Ali N., Omar F. Abdul- Rasheed, Monther F. Mahdi, and Ayad M. R. Raauf. "The Evaluation of Antiproliferative Effect of Imatinib derivatives Against Breast and Colon Cell-Lines." International Journal of Pharmaceutical Quality Assurance 11, no. 01 (2013): 74–82. http://dx.doi.org/10.25258/ijpqa.11.1.22.

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Background: Cancer is considered as one of the major leading causes of death. Tyrosine kinase inhibitors are recognized for their potential antiproliferative effects. Materials and methods: In the previous study, the authors designed, synthesized, and characterized two imatinib derivatives. These derivatives were biologically evaluated with the utilization of MCF-7, HCT116, and MDCK cell lines. Results: In respect to the imatinib standard, compound 2b has superior activity against HCT116 cell line (IC50; 15.88 μg/mL against 18.52 μg/mL for imatinib) and an improved cytotoxic activity on MDCK c

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14

Bayoumi, Hadeel M., Mayson H. Alkhatib, and Madeha N. Al-Seeni. "Carvacrol effect on topotecan cytotoxicity in various human cancer cells in vitro." Pharmacia 68, no. 2 (2021): 353–63. http://dx.doi.org/10.3897/pharmacia.68.e65878.

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Purpose: To investigate the modulatory effect of the natural phytochemical, carvacrol, on Topotecan (TOPO) cytotoxicity and cellular uptake in different cancer cell lines. Methods: The cytotoxicity of the carvacrol/TOPO combination therapy was determined in vitro using crystal violet assay. Coomassie blue and DAPI fluorescent stains were used for cellular morphology and molecular cell death assessments, respectively. Additionally, TOPO cellular uptake after carvacrol/TOPO combination therapy was determined. Results: Treatment of HeLa and HCT116 with carvacrol/TOPO resulted in 7.70- and 5.71-fo

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15

El Newahie, Aliya, Yassin Nissan, Nasser Ismail, Dalal Abou El Ella, Sohair Khojah, and Khaled Abouzid. "Design and Synthesis of New Quinoxaline Derivatives as Anticancer Agents and Apoptotic Inducers." Molecules 24, no. 6 (2019): 1175. http://dx.doi.org/10.3390/molecules24061175.

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The quinoxaline scaffold is a promising platform for the discovery of active chemotherapeutic agents. Three series of quinoxaline derivatives were synthesized and biologically evaluated against three tumor cell lines (HCT116 human colon carcinoma, HepG2, liver hepatocellular carcinoma and MCF-7, human breast adenocarcinoma cell line), in addition to VEGFR-2 enzyme inhibition activity. Compounds VIId, VIIIa, VIIIc, VIIIe and XVa exhibited promising activity against the tested cell lines and weak activity against VEGFR-2. Compound VIIIc induced a significant disruption in the cell cycle profile

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16

Pavić, Kristina, Maja Beus, Goran Poje, Lidija Uzelac, Marijeta Kralj, and Zrinka Rajić. "Synthesis and Biological Evaluation of Harmirins, Novel Harmine–Coumarin Hybrids as Potential Anticancer Agents." Molecules 26, no. 21 (2021): 6490. http://dx.doi.org/10.3390/molecules26216490.

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As cancer remains one of the major health burdens worldwide, novel agents, due to the development of resistance, are needed. In this work, we designed and synthesized harmirins, which are hybrid compounds comprising harmine and coumarin scaffolds, evaluated their antiproliferative activity, and conducted cell localization and cell cycle analysis experiments. Harmirins were prepared from the corresponding alkynes and azides under mild reaction conditions using Cu(I) catalyzed azide–alkyne cycloaddition, leading to the formation of the 1H-1,2,3-triazole ring. Antiproliferative activity of harmir

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17

Bayoumi, Hadeel M., Mayson H. Alkhatib, and Madeha N. Al-Seeni. "Carvacrol effect on topotecan cytotoxicity in various human cancer cells in vitro." Pharmacia 68, no. (2) (2021): 353–63. https://doi.org/10.3897/pharmacia.68.e65878.

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Purpose: To investigate the modulatory effect of the natural phytochemical, carvacrol, on Topotecan (TOPO) cytotoxicity and cellular uptake in different cancer cell lines. Methods: The cytotoxicity of the carvacrol/TOPO combination therapy was determined in vitro using crystal violet assay. Coomassie blue and DAPI fluorescent stains were used for cellular morphology and molecular cell death assessments, respectively. Additionally, TOPO cellular uptake after carvacrol/TOPO combination therapy was determined. Results: Treatment of HeLa and HCT116 with carvacrol/TOPO resulted in 7.70- and 5.71-fo

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18

Pawłowska, Monika, Anna Kwaśniewska, Zofia Mazerska, and Ewa Augustin. "Enhanced Activity of P4503A4 and UGT1A10 Induced by Acridinone Derivatives C-1305 and C-1311 in MCF-7 and HCT116 Cancer Cells: Consequences for the Drugs’ Cytotoxicity, Metabolism and Cellular Response." International Journal of Molecular Sciences 21, no. 11 (2020): 3954. http://dx.doi.org/10.3390/ijms21113954.

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Activity modulation of drug metabolism enzymes can change the biotransformation of chemotherapeutics and cellular responses induced by them. As a result, drug-drug interactions can be modified. Acridinone derivatives, represented here by C-1305 and C-1311, are potent anticancer drugs. Previous studies in non-cellular systems showed that they are mechanism-based inhibitors of cytochrome P4503A4 and undergo glucuronidation via UDP-glucuronosyltranspherase 1A10 isoenzyme (UGT1A10). Therefore, we investigated the potency of these compounds to modulate P4503A4 and UGT1A10 activity in breast MCF-7 a

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19

Liu, Jin-Chuan, Bo Chen, Jia-Lin Yang, Jian-Quan Weng, Qian Yu, and De-Xuan Hu. "Design, Synthesis and Cytotoxicity of Thiazole-Based Stilbene Analogs as Novel DNA Topoisomerase IB Inhibitors." Molecules 27, no. 3 (2022): 1009. http://dx.doi.org/10.3390/molecules27031009.

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A series of new thiazole-based stilbene analogs were designed, synthesized and evaluated for DNA topoisomerase IB (Top1) inhibitory activity. Top1-mediated relaxation assays showed that the synthesized compounds possessed variable Top1 inhibitory activity. Among them, (E)-2-(3-methylstyryl)-4-(4-fluorophenyl)thiazole (8) acted as a potent Top1 inhibitor with high Top1 inhibition of ++++ which is comparable to that of CPT. A possible binding mode of compound 8 with Top1–DNA complex was further provided by molecular docking. An MTT assay against human breast cancer (MCF-7) and human colon cancer

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20

Pršir, Kristina, Ema Horak, Marijeta Kralj, et al. "Design, Synthesis, Spectroscopic Characterisation and In Vitro Cytostatic Evaluation of Novel Bis(coumarin-1,2,3-triazolyl)benzenes and Hybrid Coumarin-1,2,3-triazolyl-aryl Derivatives." Molecules 27, no. 3 (2022): 637. http://dx.doi.org/10.3390/molecules27030637.

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In this work, a series of novel 1,2,3-triazolyl-coumarin hybrid systems were designed as potential antitumour agents. The structural modification of the coumarin ring was carried out by Cu(I)-catalysed Huisgen 1,3-dipolar cycloaddition of 7-azido-4-methylcoumarin and terminal aromatic alkynes to obtain 1,4-disubstituted 1,2,3-triazolyl-coumarin conjugates 2a–g, bis(1,2,3-triazolyl-coumarin)benzenes 2h–i and coumarin-1,2,3-triazolyl-benzazole hybrids 4a–b. The newly synthesised hybrid molecules were investigated for in vitro antitumour activity against five human cancer cell lines, colon carcin

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21

Krishnappa, Srinivasa, Yalpi Karthik, and Manjula Shantaram. "Augmentation of in vitro cytotoxic potentiality of crude methanolic leaf extract of Olea dioica as a pivotal anticancer source." Biomedicine 43, no. 1 (2023): 79–86. http://dx.doi.org/10.51248/.v43i1.2573.

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Introduction and Aim: Tumor is the major cause of death world-wide, with an approximate 10 million fatalities in 2020, or almost one in every six deaths. The concerns with the current commercially available anticancer medications' low selectivity and persistent side effects have driven the research of safer and more effective chemotherapeutic drugs. The current work is focused on determining the cytotoxic potential of crude methanolic extract of Olea dioica leaves against various cancer cell lines viz., A549 (human lung cancer), HCT116 (human colorectal cancer), HeLa (human cervical cancer), M

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22

Rao, Poorima BN, and Farah Deeba. "Expressions of biomarkers in MCF7 Breast and Colon Cancer Cell Lines." Journal of Drug Delivery and Therapeutics 10, no. 2 (2020): 107–14. http://dx.doi.org/10.22270/jddt.v9i4-s.3993.

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Cancer is one of the leading causes of death which accounts for 13% of total deaths, worldwide. Colorectal and Breast cancer fall under main categories according to World Health Organisation (WHO) cancer facts sheet 1. The need to understand the expression of clinical biomarkers in breast cancer and colon cancer is necessary for diagnosis and therapeutic response. In this article, the expressions of histone H1 and TP53 biomarkers were established for four different colon cancer cell lines and compared with the expressions of MCF7 cell line. The results show varied expression of Histone H1 alon

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Yong, Jianping, Xiao Wang, Xiaoyuan Wu, and Canzhong Lu. "Synthesis of a Novel Ferrocene Derivative and Cytotoxicity to A549, HCT116 and MCF-7 cell lines." Current Bioactive Compounds 13, no. 999 (2017): 1. http://dx.doi.org/10.2174/1573407213666170301145718.

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24

Zimmermann, U., B. Fluehmann, W. Born, JA Fischer, and R. Muff. "Coexistence of novel amylin-binding sites with calcitonin receptors in human breast carcinoma MCF-7 cells." Journal of Endocrinology 155, no. 3 (1997): 423–31. http://dx.doi.org/10.1677/joe.0.1550423.

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Amylin, calcitonin (CT) and calcitonin gene-related peptide (CGRP) share limited structural homology including amino-terminal ring structures linked by a disulfide bridge and amidated carboxy-termini. Here, we have compared [125I]Bolton-Hunter-[Lys1] rat amylin ([125I]amylin) binding and the stimulation of cyclic AMP accumulation by human (h) amylin, hCT and hCGRP-I in the human breast carcinoma cell lines MCF-7 and T47D, which predominantly express hCT1a and hCT1b receptor isoforms (hCTR1a, hCTR1b) at a similar total number of hCT-binding sites. In MCF-7 cells, half-maximal inhibition (IC50)

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25

Balkrishna, Das, Pokhrel, et al. "Colchicine: Isolation, LC–MS QTof Screening, and Anticancer Activity Study of Gloriosa superba Seeds." Molecules 24, no. 15 (2019): 2772. http://dx.doi.org/10.3390/molecules24152772.

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Colchicine was extracted from Gloriosa superba seeds using the Super Critical Fluid (CO2) Extraction (SCFE) technology. The seeds were purified upto 99.82% using column chromatography. Colchicine affinity was further investigated for anticancer activity in six human cancer cell lines, i.e., A549, MCF-7, MDA-MB231, PANC-1, HCT116, and SiHa. Purified colchicine showed the least cell cytotoxicity and antiproliferation and caused no G2/M arrest at clinically acceptable concentrations. Mitotic arrest was observed in only A549 and MDA-MB231 cell lines at 60nM concentration. Our finding indicated the

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26

Moreira, Joana, Patrícia M. A. Silva, Matilde Barros, et al. "Discovery of a New Chalcone-Trimethoxycinnamide Hybrid with Antimitotic Effect: Design, Synthesis, and Structure—Activity Relationship Studies." Pharmaceuticals 16, no. 6 (2023): 879. http://dx.doi.org/10.3390/ph16060879.

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In this work, the design and synthesis of a new chalcone-trimethoxycinnamide hybrid (7) based on the combination of subunits of two promising antiproliferative compounds (CM-M345 (1) and BP-M345 (2)), previously obtained by our research group, are reported. In order to expand the structure–activity relationship (SAR) knowledge, a new series of 7-analogues was also designed and synthetized. All the compounds were evaluated for their antitumor activity against melanoma (A375-C5), breast adenocarcinoma (MCF-7), and colorectal carcinoma (HCT116) cell lines, as well as non-tumor HPAEpiC cells. Thre

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27

Mohamed, Gamal A., Ali A. Alqarni, Hossam M. Abdallah, Abdelsattar M. Omar, and Sabrin RM Ibrahim. "Cytotoxic and alpha amylase-inhibitory metabolites from Tagetes minuta: In vitro evaluation and docking studies." Tropical Journal of Pharmaceutical Research 22, no. 4 (2023): 795–804. http://dx.doi.org/10.4314/tjpr.v22i4.12.

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Purpose: To investigate the cytotoxic and alpha-amylase inhibitory (AAI) potential of methanol (MeOH) extract of T. minuta and its isolated metabolites.  Methods: Phytochemical investigation of MeOH extract of the aerial parts of T. minuta was accomplished using SiO2 and Rp-18 column chromatography (CC). The structures of the isolated metabolites were determined and verified based on various data, in addition to comparison with literature data. The metabolites were assessed for cytotoxic potential against HepG2, MCF-7, and HCT116 cell lines utilizing sulphur rhodamine B (SRB) assay. The

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Tosoc, John Paul. "ID: 1012 Cytotoxicity of Corchorus olitorius Linn. aqueous leaf extract against human carcinoma cells." Biomedical Research and Therapy 4, S (2017): 86. http://dx.doi.org/10.15419/bmrat.v4is.290.

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C. olitorius are used as herbal medicine and eaten as vegetable by local people in Philippines. The T’boli tribe commonly uses this plant to treat common illnesses such as pimples, wounds, boils, and inflammations. According to studies, the leaves of C. olitorius has properties to treat demulcent, diuretic, febrifuge, chronic cystitis, dysuria and even tumor. The aim of this study is to evaluate the cytotoxicity properties of the crude aqueous extract of C. olitorius leaf against colon (HCT116), breast (MCF-7), and liver (HepG2) carcinoma cell-lines using the MTT cell proliferation assay. The

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Phaosiri, Chanokbhorn, Chavi Yenjai, Thanaset Senawong, et al. "Histone Deacetylase Inhibitory Activity and Antiproliferative Potential of New [6]-Shogaol Derivatives." Molecules 27, no. 10 (2022): 3332. http://dx.doi.org/10.3390/molecules27103332.

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Twenty newly synthesized derivatives of [6]-shogaol (4) were tested for inhibitory activity against histone deacetylases. All derivatives showed moderate to good histone deacetylase inhibition at 100 µM with a slightly lower potency than the lead compound. Most potent inhibitors among the derivatives were the pyrazole products, 5j and 5k, and the Michael adduct with pyridine 4c and benzothiazole 4d, with IC50 values of 51, 65, 61 and 60 µM, respectively. They were further evaluated for isoform selectivity via a molecular docking study. Compound 4d showed the best selectivity towards HDAC3, whe

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Konyar, Dilan, Cenk A. Andac, and Erdem Buyukbingol. "Design, Synthesis and Cytotoxic Activity of Spiro(oxindole-3-3'- pyrrolidine) Derivatives." Letters in Drug Design & Discovery 15, no. 1 (2018): 37–45. http://dx.doi.org/10.2174/1570180814666170810120634.

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Background: Spiro[pyrrolidine-3,3'-oxindole] compounds are reported to be highly bioactive natural and synthetic products. Initially, spirooxindole alkaloids were isolated from plants of the Apocynaceae and Rubiaceae families, which were found to have a common scaffold, spiro[pyrrolidine-3,3'-oxindole], exhibiting anticancer activities., we specifically aimed at the synthesis, characterization and anticancer activity of novel spiro[pyrrolidine-3,3' -oxindole] derivatives, compounds 6a-c and 7. Methods: The synthesis was initiated by Knovenegal condensation of indole-2-one with an appropriate b

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Wei, Rong-Rui, Qin-Ge Ma, Guo-Yue Zhong, Ming Yang, and Zhi-Pei Sang. "Identification of benzisoquinolinone derivatives with cytotoxicities from the leaves of Portulaca oleracea." Zeitschrift für Naturforschung C 74, no. 5-6 (2019): 139–44. http://dx.doi.org/10.1515/znc-2018-0151.

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Abstract Three new benzisoquinolinones (1–3), together with seven known benzisoquinolinone derivatives (4–10), were isolated from Portulaca oleracea for the first time. The structures of the isolated compounds (1–10) had been elucidated on the basis of extensive spectroscopic methods including ultraviolet, infrared, mass spectrometry, and nuclear magnetic resonance techniques and by comparison with data reported in the references. All isolated compounds were assayed for cytotoxicities against selected human lines in vitro by 3-(4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2-H-tetrazolium bromide ass

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Żurawska, Katarzyna, Marcin Stokowy, Patryk Kapica, et al. "Synthesis and Preliminary Anticancer Activity Assessment of N-Glycosides of 2-Amino-1,3,4-thiadiazoles." Molecules 26, no. 23 (2021): 7245. http://dx.doi.org/10.3390/molecules26237245.

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The addition of 2-amino-1,3,4-thiadiazole derivatives with parallel iodination of differently protected glycals has been achieved using a double molar excess of molecular iodine under mild conditions. The corresponding thiadiazole derivatives of N-glycosides were obtained in good yields and anomeric selectivity. The usage of iodine as a catalyst makes this method easy, inexpensive, and successfully useable in reactions with sugars. Thiadiazole derivatives were tested in a panel of three tumor cell lines, MCF-7, HCT116, and HeLa. These compounds initiated biological response in investigated tum

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Kudličková, Zuzana, Radka Michalková, Aneta Salayová, et al. "Design, Synthesis, and Evaluation of Novel Indole Hybrid Chalcones and Their Antiproliferative and Antioxidant Activity." Molecules 28, no. 18 (2023): 6583. http://dx.doi.org/10.3390/molecules28186583.

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The synthesis, anticancer, and antioxidant activities of a series of indole-derived hybrid chalcones are reported here. First, using the well-known Claisen–Schmidt condensation method, a set of 29 chalcones has been designed, synthesized, and consequently characterized. Subsequently, screening for the antiproliferative activity of the synthesized hybrid chalcones was performed on five cancer cell lines (HCT116, HeLa, Jurkat, MDA-MB-231, and MCF7) and two non-cancer cell lines (MCF-10A and Bj-5ta). Chalcone 18c, bearing 1-methoxyindole and catechol structural features, exhibited selective activ

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Elsayed, Amani, and Amany Belal. "Formulation, characterization and in-vitro evaluation of solid lipid nanoparticles for the delivery of a new anticancer agent, 1H-pyrazolo[3,4-d] pyrimidine derivative." Tropical Journal of Pharmaceutical Research 20, no. 5 (2022): 885–91. http://dx.doi.org/10.4314/tjpr.v20i5.1.

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    Purpose: To investigate the physicochemical properties and in vitro cytotoxic effect of a potent epidermal growth factor receptor-tyrosine kinase (EGFRWT-TK) inhibitor, 1H-pyrazolo [3,4-d] pyrimidine (FEP) derivative and formulated as solid lipid nanoparticles (SLNs) using stearic acid (ST) or glycerylmonostearate (GMS). Methods: The SLNs were prepared by hot homogenization and sonication method. The effect of formulation variables on particle size, zeta potential and polydispersity index (PDI) of SLNs were studied, and an optimized formulation selected. Drug-

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Elsharkawy, Eman Ramadan. "GC-MS analysis of chemical composition, cytotoxicity and antioxidant activities of essential oils of Senecio glaucus under drastic conditions." Main Group Chemistry 21, no. 1 (2022): 233–41. http://dx.doi.org/10.3233/mgc-210125.

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This study was designed to analyze essential oils by GC-MS and to evaluate the chemical composition, cytotoxic and antioxidant activity of aerial part of plant Seniso glaucus using two methods hydro distillation and organic solvent extraction. The essential oil was analyzed by GC-MS revealed the presence of 32 compounds most of them are sesquiterpene, the main component of essential oil were, Isolongifolene, 9-one (14.4%) Longiverbenone (13.5%), (+) 4-Carene (8.39 %), O-cymene, 4.64%, and thujone were 3.54%. Cytotoxic activity of essential oil was tested against four carcinoma cell lines (A549

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Bozhenko, Vladimir Konstantinovich, Tatyana Michailovna Kulinich, Elena Aleksandrovna Kudinova, Andrey Boldyrev, and Vladimir Alekseevich Solodkij. "New targeted anti CDK4/6 peptide MM-D37K." Journal of Clinical Oncology 31, no. 15_suppl (2013): e13545-e13545. http://dx.doi.org/10.1200/jco.2013.31.15_suppl.e13545.

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e13545 Background: MM-D37K is a synthetic peptide which consists of p16INK4a-specific inhibitor of complex cyclin D- CDK4 and CDK6 and cell penetrating peptide (CPP) – Antp (Penetratin). We investigated in vitro and in vivo cytotoxic, cytostatic and antitumor activity of MM-D37K. The level of cyclin A, Ki67,bax, bcl-2 and pRb phosphorylation was investigated. Full range of Toxicology tests and Pharmacokinetics experiments in mice, rats and rabbits were performed. Methods: Different cell lines (Jurcat, Raji, A549, MCF-7, Hct-116, Ht-29, HEK293) were incubated with 0.1-100 mM MM-D37K for 24-48 h

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Lu, Yi-hong, Ming-cang Chen, Fang Liu, et al. "Synthesis and Cytotoxic Activity of Novel C-23-Modified Asiatic Acid Derivatives." Molecules 25, no. 16 (2020): 3709. http://dx.doi.org/10.3390/molecules25163709.

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We selectively oxidized the C-23 hydroxyl group in an asiatic acid (AA) derivative and then, for the first time with AA, modification of the C-23 carboxyl group was conducted to synthesize a series of new AA derivatives. The evaluation of their cytotoxic activities against two human cancer cell lines (SKOV-3 and HCT116) using the MTT assay in vitro revealed a distinctive structure activity relationship (SAR) associated with the intramolecular hydrogen bonding of the amide moiety at C-23. According to the established SAR, the cytotoxic activities of four promising compounds were then evaluated

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Abo-Salem, Heba M., Abdullah A. Gibriel, Mohamed E. El Awady, and Adel H. Mandour. "Synthesis, Molecular Docking and Biological Evaluation of Novel Flavone Derivatives as Potential Anticancer Agents Targeting Akt." Medicinal Chemistry 17, no. 2 (2020): 158–70. http://dx.doi.org/10.2174/1573406416666200306115035.

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Background: Flavonoids are naturally occurring compounds with versatile healthpromoting effects against various diseases. Objective: This aim of this paper is to synthesize and evaluate the biological activity of novel flavone derivatives against cancer. Methods: A new series of 2-hydroxy-α,β-unsaturated ketones 2a-h, was synthesized via the reaction of N-substituted-indole-3-carboxaldehyde 1a-h with 2-hydroxy acetophenone in the presence of piperidine. The oxidative cyclization of 2a-h using hydrogen peroxide/KOH and/or dimethyl sulfoxide/I2 produced the corresponding 2-(N-substituted-1H-indo

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Oluwasegun, Adedokun, Epole Ntungwe, Ayinde Bunyamin, Lucilia Saraiva, Salvatore Princiotto, and Patrícia Rijo. "Celosia trigyna Linn (Cucurbitaceae) Annihilate Human Breast, Colon, and Lung Cancer Cells: Combination of Cheap Template for Anticancer Screening." International Journal of Translational Medicine 2, no. 4 (2022): 574–85. http://dx.doi.org/10.3390/ijtm2040043.

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Celosia trigyna is a well-known vegetable used in the preparation of many indigenous soups in Southwestern Nigeria. The aim of this study was to evaluate the anticancer property of C. trigyna of crude and solvent fractions using antioxidant, cytotoxic bench-top bioassays, and cancer cell line experiments. Cytotoxicity was carried out using Raniceps ranninus, Saccharomyces cerevisiae, and Sorghum bicolor models, as well as cytotoxicity studies against human breast (MCF), colon (HCT116), and lung (H460) cancer cell lines; radical scavenging potential against DPPH was likewise performed. A concen

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Jero, Mathu Albert, Sunil Jayalekshmi, Hari Neethu, S. Sanjeev Vishnu, and Jayakumaran Nair Ananthakrishnan. "Evaluation of bioactivities and importance of indole-3-carbinol in the Brassica oleracea L. var. capitata f. alba extracts." Research Journal of Biotechnology 19, no. 3 (2024): 20–30. http://dx.doi.org/10.25303/1903rjbt020030.

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Brassica oleracea L. var. capitata f. alba (Brassicaceae) is a nutrient rich leafy-headed cruciferous vegetable. The bioactivities of the various extracts such as aqueous, hexane, chloroform and methanol of this Indian cultivated vegetable have been investigated. The anticancer activity was tested in the specific cell lines (MCF-7, HCT116 and 3T3L1). The methanol and aqueous extracts showed the highest cytotoxicity found in the MCF7 cell line. The chloroform extract showed antibacterial activity against Gram-negative Escherichia coli, but not against Gram-positive Bacillus subtilis. The aqueou

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Ostrovskaya, L. A., D. B. Korman, E. I. Nekrasova, N. V. Bluhterova, Yu A. Hochenkova, and K. A. Abzaeva. "Cytotoxicity of Gold and Silver Polyacrylates for Tumor Cells." Biofizika 69, no. 6 (2024): 1224–30. https://doi.org/10.31857/s0006302924060097.

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The study of the cytotoxic activity of two polyacrylic acid-based compounds containing gold (aurumacryl) and silver (argacryl) against a panel of human tumor cell cultures (769-P, Caki-2, SK-RC-1 renal carcinoma lines, BT-474 breast carcinoma, NCI-H211 small cell lung carcinoma) was carried out in vitro. The results obtained were analyzed in comparison with the data established earlier for other cell cultures (MCF-7 breast carcinoma, A-549 lung carcinoma, HCT116 colon carcinoma, Mel Me melanoma). The IС50 cytotoxic index of drugs for the nine tested tumor cell lines ranged from 0.8 to 5.2 µg/m

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Noichan, Jirawan, Thanaset Senawong, Sarawut Tontapha, Vitttaya Amornkitbumrung, Natcha P. Suchaichit, and Panawan Moosophon. "Chemical Constituents of Goniothalamus elegans Leaves and their Anticancer Activity." Asian Journal of Chemistry 36, no. 1 (2023): 104–8. http://dx.doi.org/10.14233/ajchem.2024.30575.

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The methanol extract from the Goniothalamus elegans leaves showed potent antiproliferative effect on human cancer cells. After purification, goniothalamin (1), goniomicin C (2), pinocembirn (3), stigmasterol (4), trans-cinnamic acid (5), and benzoic acid (6) were isolated from the extract. Their structures were elucidated by spectroscopic analysis and comparison with literature data. The antiproliferative activity of compounds on cancer cell lines were determined by MMT assay and found that 1 displayed strong cytotoxicity towards human colon (HCT116), cervical (HeLa), and breast (MCF-7) cancer

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Suárez, Alírica Isabel, Katiuska Chávez, Jenny Valentina Garmendia, et al. "New Derivatives of Caracasine Acid with Anti-Leukemic Activity and Limited Effectiveness in Spheroid Cultures." Pharmaceuticals 18, no. 7 (2025): 1043. https://doi.org/10.3390/ph18071043.

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Background: The natural compounds caracasine acid (1) and its methyl ester, caracasine (2), isolated from the flowers of Croton micans, are effective against several tumor cell lines. Five semi-synthetic derivatives (3–7) were synthesized based on these structures. The study aimed to evaluate the cytotoxic activity of these compounds in 2D and spheroid cultures. Methods: The assays were performed in a panel of 12 human cell lines, 8 cancer and 4 normal cell lines. The compounds were evaluated on spheroids derived from the HCT116, HCT116 p53 knockout (p53KO), A549, and U2OS cell lines, as well

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Su, Manyun, Shenxi Chen, Xingzhong Liu, and Yuehu Pei. "Trichocladinols I-K, Oxatricyclic and Oxabicyclic Polyketides from Trichocladium opacum." Natural Product Communications 9, no. 5 (2014): 1934578X1400900. http://dx.doi.org/10.1177/1934578x1400900528.

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Three new polyketides, trichocladinols I-K (1-3) with oxabicyclic (1 and 3) and oxatricyclic (2) skeletons, together with three known metabolites, massarilactone G (4), massarigenin D (5), and rosigenin (6), were isolated from the solid-substrate fermentation cultures of the ascomycete fungus Trichocladium opacum. The structures of the new compounds were elucidated primarily by analysis of NMR data. The absolute configurations of 1-3 were deduced from circular dichroism (CD) data. Compounds 1-3 were tested for cytotoxicity against five human carcinoma cell lines, HeLa, A549, MCF-7, HCT116, and

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Park, Deok Bae, and Youngki Lee. "Anti-proliferative Activity of NVP-BEZ235, a Dual Inhibitor of PI3K and mTOR, in Colorectal Cancer Cells." Journal of Medicine and Life Science 10, no. 2 (2013): 179–83. http://dx.doi.org/10.22730/jmls.2013.10.2.179.

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In colorectal cancer diverse mutations of genes involved in signal transduction pathways for cell survival and proliferation areobserved, which have been the therapeutic targets for improvement of malignancies. The present study was undertaken toinvestigate whether NVP-BEZ235 (BEZ235), a dual inhibitor of PI3K/mTOR, shows any anti-proliferative effect on colorectal celllines harboring KRAS, and/or, PIK3CA, and/or BRAF mutations and to determine whether these mutational status affects thesensitivity of colorectal cancer cells to BEZ235. BEZ235 treatment induced growth inhibition in all four cel

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Mohamed, Magda F., Hamdi M. Hassaneen, Emad M. Elzayat, et al. "Biological Activity, Apoptotic Induction and Cell Cycle Arrest of New Hydrazonoyl Halides Derivatives." Anti-Cancer Agents in Medicinal Chemistry 19, no. 9 (2019): 1141–49. http://dx.doi.org/10.2174/1871520619666190306123658.

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Background:The hydrazonoyl halides are presently an important target in the field of medicinal chemistry. The interest in the chemistry of hydrazonoyl halides is a consequence of the fact that they undergo a wide variety of reactions which provide routes to a myriad of both heterocyclic and acyclic compounds. In addition, they have diverse biological activities such as antiviral, anthelmintic, antiarthropodal, fungicidal, herbicidal, insecticidal, pesticidal, acaricidal and miticidal Activity correlated to the presence of hydrazonoyl halides. Moreover, many applications in both industrial and

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Kasalović, Marijana P., Dušan Dimić, Sanja Jelača, et al. "Trimethyltin(IV) Bearing 3-(4-Methyl-2-oxoquinolin-1(2H)-yl)propanoate Causes Lipid Peroxidation-Mediated Autophagic Cell Death in Human Melanoma A375 Cells." Pharmaceuticals 17, no. 3 (2024): 372. http://dx.doi.org/10.3390/ph17030372.

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A novel trimethyltin(IV) complex (Me3SnL), derived from 3-(4-methyl-2-oxoquinolin-1(2H)-yl)propanoate ligand, has been synthesized and characterized by elemental microanalysis, UV/Vis spectrophotometry, FT-IR and multinuclear (1H, 13C and 119Sn) NMR spectroscopies. Furthermore, the structure of the ligand precursor HL was solved using SC-XRD (single-crystal X-ray diffraction). The prediction of UV/Vis and NMR spectra by quantum-chemical methods was performed and compared to experimental findings. The protein binding affinity of Me3SnL towards BSA was determined by spectrofluorometric titration

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Yong, Jianping, Mingxue Yang, Canzhong Lu, and Xiaoyuan Wu. "Synthesis of 1,1’-Ferrocene Diformates Bearing Isoxazole Moiety and Preliminarily Cytotoxicity to A549, HCT116 and MCF-7 Cell Lines." Letters in Drug Design & Discovery 15, no. 11 (2018): 1141–46. http://dx.doi.org/10.2174/1570180815666180306124920.

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Cho, Suh Young, Mi Kyoung Kim, Kwang-su Park, Hyunah Choo, and Youhoon Chong. "Quercetin–POC conjugates: Differential stability and bioactivity profiles between breast cancer (MCF-7) and colorectal carcinoma (HCT116) cell lines." Bioorganic & Medicinal Chemistry 21, no. 7 (2013): 1671–79. http://dx.doi.org/10.1016/j.bmc.2013.01.057.

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Ng, Teng Jia, Michelle Yee Mun Teo, Dek Shen Liew, et al. "Cytotoxic and apoptosis-inducing effects of wildtype and mutated Hydra actinoporin-like toxin 1 (HALT-1) on various cancer cell lines." PeerJ 7 (May 2, 2019): e6639. http://dx.doi.org/10.7717/peerj.6639.

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Background Hydra actinoporin like toxin -1 (HALT-1), is a small 18.5 kDa pore forming toxin derived from Hydra magnipapillata which has been shown to elicit strong haemolytic and cytolytic activity when in contact with cell membranes. Due to its cytotoxic potency, HALT-1 was further investigated for its potential as a toxin moiety candidate in immunotoxin developmental efforts, ideally as a form of targeted therapy against cancer. Methods In this study, wtHALT-1 (wild type) and its Y110A mutated binding domain counterpart (mHALT-1) were produced and evaluated for their cytotoxic and apoptotic

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