De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor

…, A Kalbakji, M Feher, R Dunn-Dufault…

Index: Schmidt, Jonathan M.; Mercure, Julie; Tremblay, Gilles B.; Page, Martine; Kalbakji, Aida; Feher, Miklos; Dunn-Dufault, Robert; Peter, Markus G.; Redden, Peter R. Journal of Medicinal Chemistry, 2003 , vol. 46, # 8 p. 1408 - 1418

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Citation Number: 39

Abstract

Although there are many estrogen receptor antagonists with improved tissue selectivity profiles compared with tamoxifen, optimal tissue selectivity has not yet been demonstrated. As such there is still a need for additional diversity and new chemical scaffolds to allow for exploration of improved tissue selectivity. Here, we describe the discovery of a novel phenanthrene scaffold for estrogen receptor ligands utilizing a ligand based de novo ...