Synthesis and Antiproliferative Activity of New Coumarin-Based Benzopyranone Derivatives Against Human Tumor Cell Lines

Musiliyu      A. Musa; Ailing      Zhou; Omowunmi      A. Sadik

doi:10.2174/157340611794859280

Abstract

The synthesis and antiproliferative activity of new coumarin-based benzopyranone derivatives containing basic amino side chain are described. The cytotoxicities against A549 and MCF-7 human cancerous cell lines were determined after 24, 48, 72h drug exposure employing MTT assay at concentrations ranging from 0-100 μM. The antiproliferative activities of these compounds were compared to tamoxifen (TAM), 4-hydroxytamoxifen (4-OHT), raloxifene (RAL), 17β- estradiol (E2) and Diethylstilbestrol (DES). In vitro results indicated that compounds 10 and 12 were the most potent showing significant inhibitory activities against these cell lines. Furthermore, their antiproliferative activity against MCF- 7 human breast cancer cell line is comparable to that of TAM, RAL and 4-OHT.

Keywords: Anticancer agents, antiproliferative agents, basic amino side chain, breast cancer, coumarin, cytotoxicity activity, lung cancer, TAM, RAL, 4-OHT, MTT assay, benzopyranone, Estrogen, IC50