Synthesis and Preliminary Biological Evaluation of Estrone Dimers

Daniel Rabouina; Valerie Perrona; Blaise N'Zemba; Atul Guptaa; Rene-C. Gaudreault; Gervais Berube

doi:10.2174/157018007780077354

ISSN: 1570-1808
E-ISSN: 1875-628X

Synthesis and Preliminary Biological Evaluation of Estrone Dimers
Authors: Daniel Rabouina¹, Valerie Perrona², Blaise N'Zemba³, Atul Guptaa⁴, Rene-C. Gaudreault⁵ and Gervais Berube⁶
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¹ Groupe de Recherche en Biopathologies Cellulaires et Moleculaires, Departement de Chimie-Biologie, Universitedu Quebec a Trois-Rivieres, C.P. 500, Trois-Rivieres,Quebec, G9A 5H7, Canada. ² Groupe de Recherche en Biopathologies Cellulaires et Moleculaires, Departement de Chimie-Biologie, Universitedu Quebec a Trois-Rivieres, C.P. 500, Trois-Rivieres,Quebec, G9A 5H7, Canada. ³ Groupe de Recherche en Biopathologies Cellulaires et Moleculaires, Departement de Chimie-Biologie, Universitedu Quebec a Trois-Rivieres, C.P. 500, Trois-Rivieres,Quebec, G9A 5H7, Canada. ⁴ Groupe de Recherche en Biopathologies Cellulaires et Moleculaires, Departement de Chimie-Biologie, Universitedu Quebec a Trois-Rivieres, C.P. 500, Trois-Rivieres,Quebec, G9A 5H7, Canada. ⁵ Groupe de Recherche en Biopathologies Cellulaires et Moleculaires, Departement de Chimie-Biologie, Universitedu Quebec a Trois-Rivieres, C.P. 500, Trois-Rivieres,Quebec, G9A 5H7, Canada. ⁶ Groupe de Recherche en Biopathologies Cellulaires et Moleculaires, Departement de Chimie-Biologie, Universitedu Quebec a Trois-Rivieres, C.P. 500, Trois-Rivieres,Quebec, G9A 5H7, Canada.
Source: Letters in Drug Design & Discovery, Volume 4, Issue 3, Apr 2007, p. 171 - 174
DOI: https://doi.org/10.2174/157018007780077354
- Available online: 01 Apr 2007

Abstract

A rapid and efficient synthesis of estrogenic dimers, with 45% overall yield, is described. The new molecules possess two estrone units linked at position 16, with either an alkyl chain or a polyethylene glycol chain. The biological activity of these compounds was evaluated in vitro on estrogen dependent and independent human breast tumor cell lines: MCF-7 and MDA-MB-231.

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2007-04-01

2025-05-28

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Article Type: Research Article

Keyword(s): 17 β-estradiol; 4-dimethylaminopyridine (DMAP); Estrogen receptor (ER); N,Ndicyclohexylcarbodiimide (DCC); Phase transfer catalysis (PTC); Polyethyleneglycol (PEG)

Synthesis and Preliminary Biological Evaluation of Estrone Dimers

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