Design, Synthesis, and Anti-Proliferative Activity of Quinoxaline Linked 1,2,4-Oxadiazole Hybrids

被引：4

作者：

Badithapuram, Vinitha ^{[1
]}

Nukala, Satheesh Kumar ^{[1
]}

Thirukovela, Narasimha Swamy ^{[1
]}

Manchal, Ravinder ^{[1
]}

Dasari, Gouthami ^{[1
]}

Bandari, Srinivas ^{[1
]}

机构：

[1] Chaitanya Deemed Univ, Dept Chem, Warangal 506001, Andhra Pradesh, India

来源：

RUSSIAN JOURNAL OF GENERAL CHEMISTRY | 2022年 / 92卷 / 01期

关键词：

quinoxaline-1; 2; 4-oxadiazole; in vitro anticancer activity; molecular docking studies; in vitro tyrosine kinase EGFR inhibitory activity; SAR studies; POTENTIAL ANTICANCER; DERIVATIVES; PHIDIANIDINE; DISCOVERY;

D O I：

10.1134/S1070363222010169

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Herein, synthesis of some new quinoxaline-1,2,4-oxadiazole derivatives is presented, and their in vitro anti-cancer activity against four human cancer cell lines like MCF-7 (human breast), HeLa (human cervical), HCT116 (human colon carcinoma) HepG2 (liver hepato cellular carcinoma) is tested. The results reveal promising results for four products. One of the products displays higher activity against all tested cell lines than the standard drug etoposide. Molecular docking studies of the products on EGFR receptor suggest that the most potent compound strongly binds to protein EGFR (pdbid: 4HJO). Two compounds exhibit promising inhibitory activity of tyrosine kinase EGFR.

引用

页码：117 / 124

页数：8

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