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

  • J Med Chem. 2008 Dec 25;51(24):8163-7. doi: 10.1021/jm8008635.
Gadarla Randheer Reddy  1 ,  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
Affiliations
  • 1. Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Road, Zhunan Town, Miaoli County 350, Taiwan, Republic of China.
PMID: 19053773 DOI: 10.1021/jm8008635
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.