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Letters in Drug Design & Discovery

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

DOI: 10.2174/157018007780077354

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Synthesis and Preliminary Biological Evaluation of Estrone Dimers

Page: [171 - 174] Pages: 4

  • * (Excluding Mailing and Handling)

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.

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