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

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• 作者：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
• 刊名：Journal of Medicinal Chemistry
• 出版年：2008
• 出版时间：December 25, 2008
• 年：2008
• 卷：51
• 期：24
• 页码：8163-8167
• 全文大小：173K
• 年卷期：v.51,no.24(December 25, 2008)
• ISSN：1520-4804

文摘

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.