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Singh, Kuldeep and Verma, Vikas and Yadav, Kavita and Sreekanth, Vedagopuram and Kumar, Devinder and Bajaj, Avinash and Kumar, Vinod (2014) Design, regioselective synthesis and cytotoxic evaluation of 2-aminoimidazole–quinoline hybrids against cancer and primary endothelial cells. European Journal of Medicinal Chemistry, 87. pp. 150-158. ISSN 02235234

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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.

Item Type: Article
Subjects: Biomedical Science
Bioengineering & Devices
Biochemical and Biophysical Sciences
Depositing User: RCB Library
Date Deposited: 30 Oct 2017 05:10
Last Modified: 30 Oct 2017 05:10
URI: http://rcb.sciencecentral.in/id/eprint/98

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