A novel estrogen receptor ligand template

…, H Hatoum-Mokdad, R Schoenleber, L Musza…

Index: Sibley, Robert; Hatoum-Mokdad, Holia; Schoenleber, Robert; Musza, Laszlo; Stirtan, William; Marrero, Diana; Carley, William; Xiao, Hong; Dumas, Jacques Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 11 p. 1919 - 1922

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Citation Number: 24

Abstract

Three synthetic routes towards a novel estrogen receptor ligand template based on a rigid bicyclo-[3.3.1]-nonene core have been investigated. The successful route employs Diels–Alder ring formation followed by trans-annular cyclization through an enolate intermediate. The prototype compound 3 exhibits potent binding at the ERβ receptor with promising selectivity against ERα, and is an agonist in MCF-7 cells. ... Subsequently, we observed that ether Figure 1 ...

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