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

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

Volume: 7 Issue: 2

Author(s): Musiliyu A. Musa, Ailing Zhou and Omowunmi A. Sadik

Affiliation:

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

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.

Cite this article as:

A. Musa Musiliyu, Zhou Ailing and A. Sadik Omowunmi, Synthesis and Antiproliferative Activity of New Coumarin-Based Benzopyranone Derivatives Against Human Tumor Cell Lines, Medicinal Chemistry 2011; 7 (2) . https://dx.doi.org/10.2174/157340611794859280