Synthesis and Structure− Activity Relationships of 2-Amino-1-aroylnaphthalene and 2-Hydroxy-1-aroylnaphthalenes as Potent Antitubulin Agents §

…, MS Coumar, CY Chang, YK Chiang…

Index: Chang, Jang-Yang; Yang, Ming-Fang; Chang, Chi-Yen; Chen, Chi-Ming; Kuo, Ching-Chuan; Liou, Jing-Ping Journal of Medicinal Chemistry, 2006 , vol. 49, # 21 p. 6412 - 6415

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Citation Number: 22

Abstract

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 ...