In vitro evaluation of the anti-estrogenic activity of hydroxyl substituted diphenylnaphthyl alkene ligands for the estrogen receptor

…, S Bhal, M Feher, R Dunn-Dufault, PR Redden

Index: Schmidt, Jonathan M.; Tremblay, Gilles B.; Plastina, Michael A.; Ma, Fupeng; Bhal, Sanjivanjit; Feher, Miklos; Dunn-Dufault, Robert; Redden, Peter R. Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 5 p. 1819 - 1828

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Citation Number: 11

Abstract

There is still a need for additional scaffolds to further explore tissue selectivity and improving efficacy of selective estrogen receptor modulators (SERMs). A series of hydroxyl substituted diphenylnaphthyl alkene ligands for the two estrogen receptors are described that arose from an initial de novo designed diphenylnaphthyl propylene ligand 1. All compounds gave Kis under 10nM when assayed in the presence of ERα. Generally these compounds had ...