Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
Email: lddd@benthamscience.org


Evaluation of In-Vivo Anti-Implantation and In-Vitro Anti-Proliferative Activities of Substituted 3-phenyl-4-phenylvinyl Benzopyranone Derivatives

Author(s): Atul Gupta, Ramesh Sharma, Anil Kumar Balapure, Govind Keshri, M. M. Singh, Suprabhat Ray.


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

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Article Details

Year: 2009
Page: [46 - 50]
Pages: 5
DOI: 10.2174/157018009787158508