Synthesis and Preliminary Biological Evaluation of Estrone Dimers
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)
Rights & PermissionsPrintExport