2. Academic Validation
  3. Synthesis and structure-activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution

Synthesis and structure-activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution

  • J Enzyme Inhib Med Chem. 2005 Apr;20(2):165-77. doi: 10.1080/14756360500043448.
Sylvain Gauthier 1,  Julie Cloutier,  Yves L Dory,  Alexandre Favre,  Josée Mailhot,  Carl Ouellet,  Annette Schwerdtfeger,  Yves Mérand,  Céline Martel,  Jacques Simard,  Fernand Labrie
Affiliations

Affiliation

  • 1 Oncology and Molecular Endocrinology Research Center, Laval University Medical Center (CHUL), Québec G1V 4G2, Canada. sylvain.gauthier@crchul.ulaval.ca
PMID: 15968821 DOI: 10.1080/14756360500043448
Abstract

EM-652 (acolbifene) analogs have been synthesized as selective Estrogen Receptor modulators. Substitution on the nitrogen atom of these 2H-1-benzopyran derivatives has been studied for its influence on antiestrogenic activity. Binding to the rat Estrogen Receptor, inhibition of estradiol-stimulated proliferation of T-47D breast Cancer cells, as well as antiuterotrophic and uterotrophic activities in ovariectomized mice have been evaluated. 2H-1-Benzopyran 1b (EM-343, racemic form of EM-652), which contains a piperidine ring, shows the best pharmacological profile; RBA = 380, IC50 value = 0.110 nM (in T-47D cells), as well as 63% and 84% antiuterotrophic inhibitions at the 7.5 and 75 nmol doses, respectively.

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