Selective estrogen receptor modulators with conformationally restricted side chains. Synthesis and structure-activity relationship of ERα-selective …

…, C Halleux, J Kallen, H Keller, P Ramage

Index: Renaud, Johanne; Bischoff, Serge Francois; Buhl, Thomas; Floersheim, Philipp; Fournier, Brigitte; Geiser, Martin; Halleux, Christine; Kallen, Joerg; Keller, Hansjoerg; Ramage, Paul Journal of Medicinal Chemistry, 2005 , vol. 48, # 2 p. 364 - 379

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Citation Number: 58

Abstract

We disclose herein the discovery of estrogen receptor α (ERα) selective estrogen receptor modulators (SERMs) of the tetrahydroisoquinoline series that incorporate novel conformationally restricted side chains as replacement of the aminoethoxy residue typical of SERMs. Molecular modeling studies used in conjunction with the X-ray crystal structure of the ERα ligand binding domain (LBD) with raloxifene (7) suggested a diazadecaline ...

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