國家衛生研究院 NHRI:Item 3990099045/6815

NHRI > Institute of Biotechnology and Pharmaceutical Research > Hsing-Pang Hsieh > Conference Papers/Meeting Abstract > Item 3990099045/6815

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Title:	Concise synthesis and structure-activity relationships of combretastatin A-4 analogues, 1-aroylindoles and 3-aroylindoles, as novel classes of potent antitubulin agents
Authors:	Hsieh, HP;Liou, JP;Chang, YL;Lee, SJ
Contributors:	Institute of Biotechnology and Pharmaceutical Research
Abstract:	The synthesis and study of structure-activity relationship of two new classes of synthetic antitubulin compounds based on 1-aroylindole and 3-aroylindole skeleton are described. Lead compounds 3, 10 and 14 displayed potent cytotoxicity with IC50 = 0.9 to 22 nM against human NUGC3 stomach, MKN45 stomach, MESSA uterine, A549 lung, and MCF-7 breast carcinoma cell lines. The inhibition of proliferation correlated with in vitro polymerization inhibitory activities. Structure-activity relationships revealed that 6-methoxy substitution of 3-aroylindoles and 5-methoxy substitution of 1-aroylindoles contributes to a significant extent for maximal activity by mimicking the para substitution of the methoxy group to the carbonyl group in case of aminobenzophenones. Addition of a methyl group at the C-2 position on indole ring exerts increased potency. 3,4,5-Trimethoxybenzoyl moiety was necessary for better activity, but not essential and can be replaced by 3,5-dimethoxybenzoyl and 3,4,5-trimethoxybenzyl moieties. We conclude that 1- and 3-aroylindoles constitute an interesting new class of antitubulin agents with the potential to be clinically developed for cancer treatment.
Date:	2004-08-22
Relation:	Abstracts of Papers - American Chemical Society. 2004 Aug 22;228:U924.
Link to:	http://oasys2.confex.com/acs/228nm/techprogram/P756903.HTM
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000223712803928
Appears in Collections:	[Hsing-Pang Hsieh] Conference Papers/Meeting Abstract [Shiow-Ju Lee] Conference Papers/Meeting Abstract

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