Nonsteroidal estrogen receptor isoform-selective biphenyls,Chemical Biology & Drug Design

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Nonsteroidal estrogen receptor isoform-selective biphenyls
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2017-11-10 06:21:15 , DOI: 10.1111/cbdd.13126
Seema Bhatnagar ₁ , Anjali Soni ₂ , Swati Kaushik _{1,

3} , Megha Rikhi ₁ , Thankayyan Retnabai Santhoshkumar ₃ , Bhyravabhotla Jayaram _{2,

4}

Affiliation

Novel substituted biphenyl-2,6-diethanones are designed and synthesized targeting ERα isoform. MD simulations along with MM-GBSA accounted for the binding selectivity of 3b toward ERα over ERβ. Cotreatment and E-screen studies indicated the ERα selective nature of 3b and anti-estrogenicity. ERα siRNA silencing experiments further confirmed the isoform selectivity.

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