Design, regioselective synthesis and cytotoxic evaluation of 2-aminoimidazole-quinoline hybrids against cancer and primary endothelial cells

被引：30

作者：

Singh, Kuldeep ^{[1
,3
]}

Verma, Vikas ^{[1
]}

Yadav, Kavita ^{[2
]}

Sreekanth, Vedagopuram ^{[2
]}

Kumar, Devinder ^{[1
]}

Bajaj, Avinash ^{[2
]}

Kumar, Vinod ^{[3
]}

机构：

[1] Guru Jambheshwar Univ Sci & Technol, Dept Chem, Hisar 125001, Haryana, India

[2] Reg Ctr Biotechnol, Lab Nanotechnol & Chem Biol, Gurgaon 122016, Haryana, India

[3] MM Univ, Dept Chem, Ambala 133207, Haryana, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 87卷

关键词：

Regioselectivity; 2-Aminoimidazole; Quinoline; Cytotoxicity; Selective anticancer agents; NATURAL-PRODUCTS; ALKALOIDS; ANTAGONIST; SPONGES; GROWTH; AGENTS;

D O I：

10.1016/j.ejmech.2014.09.055

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In search of new selective anti-cancer agents, a series of sixteen novel 2-aminoimidazole quinoline hybrid compounds (5a-5p) have been designed and synthesized regioselectively. We have characterized the compounds extensively using IR, 1D and 2D NMR Spectroscopy and mass spectrometry. The cytotoxicity studies against different cancer cell lines showed that the compound 5a (Imd-Ph) emerged as a potent cytotoxic scaffold. Imd-Ph (5a) exhibited a selective anticancer activity against human colon cancer cell line (HCT-116, DLD-1) and was found relatively non-toxic to breast cancer cells (MDA-MB-231) as well as to normal primary endothelial cells (HUVEC). Structure-activity relationship of imidazole -quinoline hybrid scaffolds revealed differential and selective toxicities exerted by the different derivatives against cancer and normal cells. Structural modification of the scaffold with library of a wide variety of substituents may lead to the development of novel selective anti-cancer agents in the future. (C) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：150 / 158

页数：9

共 37 条

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