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:Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow-226001, India.
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.
