Design, synthesis and bioevaluation of novel candidate selective estrogen receptor modulators

…, A Bhattacharyya, VS Parmar, J Balzarini…

Index: Yadav, Yogesh; MacLean, Erin D.; Bhattacharyya, Annyt; Parmar, Virinder S.; Balzarini, Jan; Barden, Christopher J.; Too, Catherine K.L.; Jha, Amitabh European Journal of Medicinal Chemistry, 2011 , vol. 46, # 9 p. 3858 - 3866

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Citation Number: 10

Abstract

In an systematic attempt to develop novel Selective Estrogen Receptor Modulators (SERMs), chiral 1-((4-(2-(dialkylamino) ethoxy) phenyl)(2-hydroxynaphthalen-1-yl) methyl) piperidin-4- ols were designed based on an accepted pharmacophore model. Simpler prototypes, viz. racemic 1-((2-hydroxynaphthalen-1-yl) arylmethyl) piperidin-4-ols, were first synthesized to develop kinetic resolution to pure enantiomers. Simultaneously, a series of racemic 1-((4-( ...