Synthesis and Structure−Activity Relationships of 2-Amino-1-aroylnaphthalene and 2-Hydroxy-1-aroylnaphthalenes as Potent Antitubulin Agents
Journal of Medicinal Chemistry2008Vol. 51(24), pp. 8163–8167
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G. 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
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 IC(50) 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.
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