Synthesis of 17β-estradiol platinum(II) complexes: biological evaluation on breast cancer cell lines

The synthesis of a novel series of 17β-estradiol-linked platinum(II) complexes is described. The new molecules are linked with an alkyl chain at position 16α of the steroid nucleus and bear a 16β-hydroxymethyl side chain. They are made from estrone in five chemical steps with an overall yield exceeding 28%. The biological activity of these compounds was evaluated in vitro on estrogen dependent and independent (ER+ and ER−) human breast cancers. The derivatives incorporating a 2-(2′-aminoethyl)pyridine ligand displayed good activity against the cell lines particularly when the connecting arm is 10 carbon atoms long.