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

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24 Citations (Scopus)

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 comparable tubulin binding efficacy as that of colchicine.

Original languageEnglish
Pages (from-to)8163-8167
Number of pages5
JournalJournal of Medicinal Chemistry
Volume51
Issue number24
DOIs
Publication statusPublished - Dec 25 2008

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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    Reddy, G. R., Kuo, C-C., Tan, U-K., Coumar, M. S., Chang, C-Y., Chiang, Y-K., Lai, M-J., Yeh, J-Y., Wu, S-Y., Chang, J-Y., Liou, J. P., & Hsieh, H-P. (2008). Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents. Journal of Medicinal Chemistry, 51(24), 8163-8167. https://doi.org/10.1021/jm8008635