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 language | English |
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Pages (from-to) | 6046-6056 |
Number of pages | 11 |
Journal | European Journal of Medicinal Chemistry |
Volume | 46 |
Issue number | 12 |
DOIs | |
Publication status | Published - 2011 Dec |
All Science Journal Classification (ASJC) codes
- Pharmacology
- Drug Discovery
- Organic Chemistry