Abstract
A series of substituted 3-phenyl-4-phenylvinyl benzopyranone derivatives (11a-e) was evaluated for their antiimplantation activity in mature female Sprague-Dawley rat model. Compounds were further evaluated for antiproliferative activity in human adenocarcenoma breast cancer cell line (MCF-7 cancer cell line). The tested compounds showed significant anti-proliferative activity with moderate anti-implantation activity. The inhibitory concentration (IC50) values of most active compounds 11 (c-e) are 8.43 μM, 7.97 μM and 7.91 μM respectively and comparable to that of tamoxifen (5.10 μM), a well known antiestrogen used for treatment of breast cancer.
Keywords: Anti-implantation agents, Estrogen receptors, Estrogen agonists, Estrogen antagonists, Fertility regulation, Antiproliferative agents, Drug Research
Letters in Drug Design & Discovery
Title: Evaluation of In-Vivo Anti-Implantation and In-Vitro Anti-Proliferative Activities of Substituted 3-phenyl-4-phenylvinyl Benzopyranone Derivatives
Volume: 6 Issue: 1
Author(s): Atul Gupta, Ramesh Sharma, Anil Kumar Balapure, Govind Keshri, M. M. Singh and Suprabhat Ray
Affiliation:
Keywords: Anti-implantation agents, Estrogen receptors, Estrogen agonists, Estrogen antagonists, Fertility regulation, Antiproliferative agents, Drug Research
Abstract: A series of substituted 3-phenyl-4-phenylvinyl benzopyranone derivatives (11a-e) was evaluated for their antiimplantation activity in mature female Sprague-Dawley rat model. Compounds were further evaluated for antiproliferative activity in human adenocarcenoma breast cancer cell line (MCF-7 cancer cell line). The tested compounds showed significant anti-proliferative activity with moderate anti-implantation activity. The inhibitory concentration (IC50) values of most active compounds 11 (c-e) are 8.43 μM, 7.97 μM and 7.91 μM respectively and comparable to that of tamoxifen (5.10 μM), a well known antiestrogen used for treatment of breast cancer.
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Cite this article as:
Gupta Atul, Sharma Ramesh, Balapure Kumar Anil, Keshri Govind, Singh M. M. and Ray Suprabhat, Evaluation of In-Vivo Anti-Implantation and In-Vitro Anti-Proliferative Activities of Substituted 3-phenyl-4-phenylvinyl Benzopyranone Derivatives, Letters in Drug Design & Discovery 2009; 6 (1) . https://dx.doi.org/10.2174/157018009787158508
DOI https://dx.doi.org/10.2174/157018009787158508 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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