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

doi:10.1021/jm900060s

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
卷	52
發行號	15
DOIs	https://doi.org/10.1021/jm900060s
出版狀態	已發佈 - 8月 13 2009

ASJC Scopus subject areas

分子醫學
藥物發現

UN SDG

此研究成果有助於以下永續發展目標

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10.1021/jm900060s

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Wu, Y. S., Coumar, M. S., Chang, J. Y., Sun, H. Y., Kuo, F. M., Kuo, C. C., Chen, Y. J., Chang, C. Y., Hsiao, C. L., Liou, J. P., Chen, C. P., Yao, H. T., Chiang, Y. K., Tan, U. K., Chen, C. T., Chu, C. Y., Wu, S. Y., Yeh, T. K., Lin, C. Y., & Hsieh, H. P. (2009). Synthesis and evaluation of 3-aroylindoles as anticancer agents: Metabolite approach. Journal of Medicinal Chemistry, 52(15), 4941-4945. https://doi.org/10.1021/jm900060s

Synthesis and evaluation of 3-aroylindoles as anticancer agents : Metabolite approach. / Wu, Yu Shan; Coumar, Mohane Selvaraj; Chang, Jang Yang; Sun, Hsu Yi; Kuo, Fu Ming; Kuo, Ching Chuan; Chen, Ying Jun; Chang, Chi Yen; Hsiao, Chia Ling; Liou, Jing Ping; Chen, Ching Ping; Yao, Hsien Tsung; Chiang, Yi Kun; Tan, Uan Kang; Chen, Chiung Tong; Chu, Chang Ying; Wu, Su Ying; Yeh, Teng Kuang; Lin, Chin Yu; Hsieh, Hsing Pang.

於: Journal of Medicinal Chemistry, 卷 52, 編號 15, 13.08.2009, p. 4941-4945.

研究成果: 雜誌貢獻 › 文章 › 同行評審

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 2009, 'Synthesis and evaluation of 3-aroylindoles as anticancer agents: Metabolite approach', Journal of Medicinal Chemistry, 卷 52, 編號 15, 頁 4941-4945. https://doi.org/10.1021/jm900060s

Wu, Yu Shan ; Coumar, Mohane Selvaraj ; Chang, Jang Yang ; Sun, Hsu Yi ; Kuo, Fu Ming ; Kuo, Ching Chuan ; Chen, Ying Jun ; Chang, Chi Yen ; Hsiao, Chia Ling ; Liou, Jing Ping ; Chen, Ching Ping ; Yao, Hsien Tsung ; Chiang, Yi Kun ; Tan, Uan Kang ; Chen, Chiung Tong ; Chu, Chang Ying ; Wu, Su Ying ; Yeh, Teng Kuang ; Lin, Chin Yu ; Hsieh, Hsing Pang. / Synthesis and evaluation of 3-aroylindoles as anticancer agents : Metabolite approach. 於: Journal of Medicinal Chemistry. 2009 ; 卷 52, 編號 15. 頁 4941-4945.

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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.",

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

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AU - Kuo, Fu Ming

AU - Kuo, Ching Chuan

AU - Chen, Ying Jun

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AU - Hsiao, Chia Ling

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AU - Chen, Ching Ping

AU - Yao, Hsien Tsung

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AU - Tan, Uan Kang

AU - Chen, Chiung Tong

AU - Chu, Chang Ying

AU - Wu, Su Ying

AU - Yeh, Teng Kuang

AU - Lin, Chin Yu

AU - Hsieh, Hsing Pang

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

摘要

ASJC Scopus subject areas

UN SDG

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