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

Research output: Contribution to journalArticlepeer-review

26 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 - 2008 Dec 25

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery

Fingerprint Dive into the research topics of 'Synthesis and structure-activity relationships of 2-amino-1- aroylnaphthalene and 2-hydroxy-1-aroylnaphthalenes as potent antitubulin agents'. Together they form a unique fingerprint.

Cite this