Synthesis and biological evaluation of 2,3,4-triarylbenzopyran derivatives as SERM and therapeutic agent for breast cancer |
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| Authors: | Shailesh Kumar Shreekant Deshpande Vishal Chandra Shakti Kitchlu Anila Dwivedi Vadithe Lakshma Nayak Rituraj Konwar Yenamandra S Prabhakar Devi Prasad Sahu |
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| Institution: | 1. Medicinal and Process Chemistry Division, Central Drug Research Institute, Lucknow 226001, India;2. Endocrinology Division, Central Drug Research Institute, Lucknow 226001, India |
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| 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 IC50 at 6.97 μM against MCF-7 and 11f showed the lowest IC50 value of 5.6 μM 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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