Design, synthesis and in vitro anticancer activity of novel quinoline and oxadiazole derivatives of ursolic acid.

Related Articles

Design, synthesis and in vitro anticancer activity of novel quinoline and oxadiazole derivatives of ursolic acid.

Bioorg Med Chem Lett. 2017 Jul 12;:

Authors: Gu W, Jin XY, Li DD, Wang SF, Tao XB, Chen H

Abstract
A series of new quinoline derivatives of ursolic acid were designed and synthesized in an attempt to develop potential anticancer agents. The structures of these compounds were identified by (1)H NMR, (13)C NMR, IR and ESI-MS spectra analysis. The target compounds were evaluated for their in vitro cytotoxicity against three human cancer cell lines (MDA-MB-231, Hela and SMMC-7721). From the results, compounds 3a-d displayed significant antitumor activity against three cancer cell lines. Especially, compound 3b was found to be the most potent derivative with IC50 values of 0.61±0.07, 0.36±0.05, 12.49±0.08μM against MDA-MB-231, HeLa and SMMC-7721 cells, respectively, stronger than positive control etoposide. Furthermore, the Annexin V-FITC/PI dual staining assay revealed that compound 3b could significantly induce the apoptosis of MDA-MB-231 cells in a dose-dependent manner. The cell cycle analysis also indicated that compound 3b could cause cell cycle arrest of MDA-MB-231 cells at G0/G1 phase.

PMID: 28733083 [PubMed - as supplied by publisher]

http://ift.tt/2uXKXiv