國家衛生研究院 NHRI:Item 3990099045/3746

NHRI > Institute of Biotechnology and Pharmaceutical Research > Hsing-Pang Hsieh > Periodical Articles > Item 3990099045/3746

Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/3746

Title:	Synthesis and evaluation of 3-aroylindoles as anticancer agents: Metabolite approach
Authors:	Wu, YS;Coumar, MS;Chang, JY;Sun, HY;Kuo, FM;Kuo, CC;Chen, YJ;Chang, CY;Hsiao, CL;Liou, JP;Chen, CP;Yao, HT;Chiang, YK;Tan, UK;Chen, CT;Chu, CY;Wu, SY;Yeh, TK;Lin, CY;Hsieh, HP
Contributors:	Division of Biotechnology and Pharmaceutical Research;National Institute of Cancer Research
Abstract:	BPR0L075 (2) is a potential anticancer drug candidate designed from Combretastatin A-4 (1) based on the bioisosterismprinciple.Metabolites of 2, proposed from in vitrohumanmicrosome studies,were synthesized, leading to the identification of metabolite-derived analogue 10 with 40-350 pM potency against various cancer cell lines. Insights gained from the major inactive metabolite of 2 led to the development of 29, with better pharmacokinetics and improved potency in the tumor xenograft model than 2.
Date:	2009-08-13
Relation:	Journal of Medicinal Chemistry. 2009 Aug 13;52(15):4941-4945.
Link to:	http://dx.doi.org/10.1021/jm900060s
JIF/Ranking 2023:	http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=0022-2623&DestApp=IC2JCR
Cited Times(WOS):	https://www.webofscience.com/wos/woscc/full-record/WOS:000268661600037
Cited Times(Scopus):	http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=68549135156
Appears in Collections:	[Hsing-Pang Hsieh] Periodical Articles [Jang-Yang Chang] Periodical Articles [Teng-Kuang Yeh] Periodical Articles [Su-Ying Wu] Periodical Articles [Chiung-Tong Chen] Periodical Articles [Ching-Chuan Kuo] Periodical Articles

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