Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel 1,2,3-Triazole Tagged 5-[(1H-Indol-3-yl)methylene]pyrimidine-2,4,6(1H,3H,5H)trione Derivatives

被引：9

作者：

Kumar, Ashok ^{[1
,4
]}

Kumar, B. Sathish ^{[2
]}

Sreenivas, E. ^{[3
]}

Subbaiah, T. ^{[4
]}

机构：

[1] Sreenidhi Inst Sci & Technol, Dept Chem, Hyderabad 501301, Telangana, India

[2] Osmania Univ, Dept Chem, Hyderabad 500007, Telangana, India

[3] Averin Biotech Pvt Ltd Windsorplaza, Bioinformat Div, Hyderabad 500044, Telangana, India

[4] Koneru Lakshmaiah Deemed Be Univ, Dept Chem, Vaddeswaram 522502, Andhra Pradesh, India

来源：

RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2018年 / 88卷 / 03期

关键词：

1,2,3-triazole; indole; click reaction; cervical cancer; molecular docking; MYCOBACTERIUM-TUBERCULOSIS; ANTICONVULSANT ACTIVITY; ANTIMICROBIAL ACTIVITY; INHIBITORY-ACTIVITY; ANTIVIRAL ACTIVITY; INDOLE; ANTIBACTERIAL; HETEROCYCLES; ANALOGS; DESIGN;

D O I：

10.1134/S1070363218030313

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Novel 5-{(1-[(1-phenyl-1H-1,2,3-triazol-4-yl)methyl]-1H-indol-3-yl)methylene}pyrimidine-2,4,6-(1H,3H,5H)trione derivatives (5a-5k) were synthesized by the click reaction. All compounds 5a-5k were characterized by H-1 and C-13 NMR, IR and Mass spectra and evaluated for their in vitro anticancer activity against cervical cancer cell lines. Among all, compound 5e (IC50 = 6.76 mu M), shown high inhibitory activity. Docking analysis of all the compounds with the Lipid kinase PI3K-alpha revealed that the compound 5e fitted well in the active site pocket, showing the best docking score (LibDock) of 123.274.

引用

页码：587 / 595

页数：9

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