In-vitro Antiproliferative Activity of Benzopyranone Derivatives in Comparison with Standard Chemotherapeutic Drugs

✍ Scribed by Musiliyu A. Musa; John S. Cooperwood; M. Omar F. Khan; Taufiq Rahman

• Publisher: John Wiley and Sons
• Year: 2010
• Tongue: English
• Weight: 317 KB
• Volume: 344
• Category: Article
• ISSN: 0365-6233
• DOI: 10.1002/ardp.201000207

✦ Synopsis

Abstract

The cytotoxic activities of five new benzopyranone derivatives containing basic amino side chain are described. Their cytotoxicities against ER(+) MCF‐7 and ER(–) MDA‐MB‐231 human breast cancer cell lines, and Ishikawa human endometrial cell line were determined after 72 h drug exposure employing CellTiter‐Glo assay at concentrations ranging from 0.01–1.0 × 10^5^ nM. The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4‐hydroxytamoxifen (4‐OHT, active metabolite of tamoxifen), and raloxifene (RAL). In‐vitro results indicated that compounds 9, 10, 12, and 13 were more potent than TAM against the human breast cancer cell lines with IC~50~ < 20 µM. The in‐silico structure–activity relationships of these compounds and their binding mode within the estrogen receptor (ER) binding site using AutoDock vina are discussed.