Synthesis and evaluation of 3-aroylindoles as anticancer agents: Metabolite approach

Yu Shan Wu, Mohane Selvaraj Coumar, Jang Yang Chang, Hsu Yi Sun, Fu Ming Kuo, Ching Chuan Kuo, Ying Jun Chen, Chi Yen Chang, Chia Ling Hsiao, Jing Ping Liou, Ching Ping Chen, Hsien Tsung Yao, Yi Kun Chiang, Uan Kang Tan, Chiung Tong Chen, Chang Ying Chu, Su Ying Wu, Teng Kuang Yeh, Chin Yu Lin, Hsing Pang Hsieh

研究成果: 雜誌貢獻文章同行評審

87 引文 斯高帕斯(Scopus)

摘要

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.

原文英語
頁(從 - 到)4941-4945
頁數5
期刊Journal of Medicinal Chemistry
52
發行號15
DOIs
出版狀態已發佈 - 8月 13 2009

ASJC Scopus subject areas

  • 分子醫學
  • 藥物發現

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