Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents

Gadarla Randheer Reddy, Ching-Chuan Kuo, Uan-Kang Tan, Mohane Selvaraj Coumar, Chi-Yen Chang, Yi-Kun Chiang, Mei-Jung Lai, Jiann-Yih Yeh, Su-Ying Wu, Jang-Yang Chang, Jing Ping Liou, Hsing-Pang Hsieh

研究成果: 雜誌貢獻文章同行評審

28 引文 斯高帕斯(Scopus)

摘要

A series of aroylnaphthalene derivatives were prepared as bioisosteres of combrestatin A-4 and evaluated for anticancer activity. 2-Amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalene, 9 and 8, respectively, showed strong antiproliferative activity with IC50 values of 2.1-26.3 nM against a panel of human cancer cell lines including multiple-drug resistant cell line. Compound 9 demonstrated better antiproliferative activity and has a comparable tubulin binding efficacy as that of colchicine.

原文英語
頁(從 - 到)8163-8167
頁數5
期刊Journal of Medicinal Chemistry
51
發行號24
DOIs
出版狀態已發佈 - 12月 25 2008

ASJC Scopus subject areas

  • 分子醫學
  • 藥物發現

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