Design, Synthesis, Evaluation and Molecular Docking Studies of Novel Triazole Linked 1,4-Dihydropyridine-isatin Scaffolds as Potent Anticancer Agents

被引：14

作者：

Deswal, Nidhi ^{[1
]}

Shrivastava, Ankita ^{[2
]}

Hossain, Md Summon ^{[2
]}

Gahlyan, Parveen ^{[1
]}

Bawa, Rashim ^{[1
]}

Gupta, Rinkoo Devi ^{[2
]}

Kumar, Rakesh ^{[1
]}

机构：

[1] Univ Delhi, Dept Chem, Bioorgan Lab, New Delhi 110007, India

[2] South Asian Univ, Fac Life Sci & Biotechnol, New Delhi 110021, India

来源：

CHEMISTRYSELECT | 2021年 / 6卷 / 04期

关键词：

Anticancer agents; isatin; 1; 4-dihydropyridine; triazole; molecular docking; CLICK CHEMISTRY; CARCINOMA; TUBULIN; CYTOTOXICITY; INHIBITORS; APOPTOSIS; TARGET; CDK2;

D O I：

10.1002/slct.202003948

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of novel triazole linked isatin-dihydropyridine hybrids (N1-N15) have been synthesized and examined for their anti proliferative activity against human cancer cell lines viz. HeLa, Huh-7, PC-3, IMR-32 and MCF-7. All of the synthesized hybrids have shown moderate to potent cytotoxicity against all the tested cell lines except IMR-32. Compounds N1, N2 and N13 have displayed an enhanced inhibitory potency against Huh-7 cell line as compared to the standard drug, doxorubicin. Out of the three, N2 has shown the highest in vitro inhibitory action with IC50 values of 6.73 +/- 0.33 mu M and 17.94 +/- 0.23 mu M against Huh-7 and MCF-7 cell lines, respectively. The docking studies of these most potent compounds have also been investigated which identified that N2 might be an excellent drug-like candidate worthy of further pursuit.

引用

页码：717 / 725

页数：9

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