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ID: ALA1152595

Journal: Bioorg Med Chem

Title: Synthesis and biological evaluation of 2,3,4-triarylbenzopyran derivatives as SERM and therapeutic agent for breast cancer.

Authors: Kumar S, Deshpande S, Chandra V, Kitchlu S, Dwivedi A, Nayak VL, Konwar R, Prabhakar YS, Sahu DP.

Abstract: A novel class of 2,3,4-triarylbenzopyrans has been synthesized and were evaluated for their selective estrogen receptor modulation activity and as a therapeutic agent for breast cancer. Among the compounds synthesized, compounds 11a and 12c exhibited 73.91% and 69.24% inhibition as estrogen antagonistic activity, respectively. Compound 12a showed the lowest IC(50) at 6.97 microM against MCF-7 and 11f showed the lowest IC(50) value of 5.6 microM against MDA-MB-231 cell line in spite of their low receptor binding affinity implicating these compounds probably act through ER independent mechanism.

CiteXplore: 19740667

DOI: 10.1016/j.bmc.2009.08.034