Synthesis and Preliminary Biological Evaluation of Estrone Dimers

Title: Synthesis and Preliminary Biological Evaluation of Estrone Dimers

Volume: 4 Issue: 3

Author(s): Daniel Rabouina, Valerie Perrona, Blaise N'Zemba, Atul Guptaa, Rene-C. Gaudreault and Gervais Berube

Affiliation:

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

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.

Cite this article as:

Rabouina Daniel, Perrona Valerie, N'Zemba Blaise, Guptaa Atul, Gaudreault Rene-C. and Berube Gervais, Synthesis and Preliminary Biological Evaluation of Estrone Dimers, Letters in Drug Design & Discovery 2007; 4 (3) . https://dx.doi.org/10.2174/157018007780077354