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
Medicinal Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/157340611794859280 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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Carbohydrates are the most essential organic molecules and are involved in the maintenance of various physiological and metabolic processes in living organisms. Carbohydrate-based compounds have come to the attention of researchers because of their significant contributions to biological functions, such as cell development and cell proliferation, connections between several cells, ...read more
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