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

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

  • Bioorg Med Chem. 2009 Oct 1;17(19):6832-40. doi: 10.1016/j.bmc.2009.08.034.
Shailesh Kumar 1,  Shreekant Deshpande,  Vishal Chandra,  Shakti Kitchlu,  Anila Dwivedi,  Vadithe Lakshma Nayak,  Rituraj Konwar,  Yenamandra S Prabhakar,  Devi Prasad Sahu
Affiliations

Affiliation

  • 1 Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India.
PMID: 19740667 DOI: 10.1016/j.bmc.2009.08.034
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.

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