Synthesis and in vitro anticancer activity of 6,7-methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-one analogs

Chien Ting Chen, Mei Hua Hsu, Yung Yi Cheng, Chin Yu Liu, Li Chen Chou, Li Jiau Huang, Tian Shung Wu, Xiaoming Yang, Kuo Hsiung Lee, Sheng Chu Kuo

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32 Citations (Scopus)

Abstract

6,7-Methylenedioxy (or 5-hydroxy-6-methoxy)-2-(substituted selenophenyl)quinolin-4-ones and their isosteric compounds were synthesized and evaluated for anticancer activity. Structure-activity relationships (SAR) of these compounds were established. Among all tested compounds, 6,7-methylenedioxy-2-(5-methylselenophen-2-yl)quinolin-4-one (4d) was found to be the most promising anticancer agent. In screening against NCI's 60 human tumor cell line panel, 4d exhibited highly selective and potent inhibitory activity against MDA-MB-435 melanoma. Furthermore, the results of COMPARE analysis suggested that 4d is an antimitotic agent with a different mechanism of action from the conventional antimitotic agents, such as colchicine, vinca alkaloids and paclitaxel. Therefore, 4d was identified as a new lead compound that merits further optimization.

Original languageEnglish
Pages (from-to)6046-6056
Number of pages11
JournalEuropean Journal of Medicinal Chemistry
Volume46
Issue number12
DOIs
Publication statusPublished - 2011 Dec

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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