4, 4′-Unsymmetrically substituted 3, 3′-biphenyl alpha helical proteomimetics as potential coactivator binding inhibitors

…, CY Chang, DP McDonnell, RN Hanson

Index: Weiser, Patrick T.; Chang, Ching-Yi; McDonnell, Donald P.; Hanson, Robert N. Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 2 p. 917 - 926

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Citation Number: 4

Abstract

Abstract A series of unsymmetrically substituted biphenyl compounds was designed as alpha helical proteomimetics with the aim of inhibiting the binding of coactivator proteins to the nuclear hormone receptor coactivator binding domain. These compounds were synthesized in good overall yields in seven steps starting from 2-bromoanisole. The final products were evaluated using cotransfection reporter gene assays and mammalian two- ...