The development of resistance to endocrine therapy as well as chemotherapy is presently a major problem in the treatment of breast cancer. To minimize this obstacle, new, more selective and potent, chemotherapeutic agents should be designed. One way to improve selectivity is to link a cytotoxic moiety to a molecule possessing an affinity to the estrogen receptor (ER). The latter would be used to direct the cytotoxic portion of the molecule towards the target cells. Our initial approach led us to the synthesis of new triphenylethylene–platinum(II) complexes 1a–c. The commercially available desoxyanisoin (10) was efficiently transformed in seven steps into the platinum(II) complexes 1a–c with an overall yield exceeding 30%. The biological activity of compounds 1a–c was evaluated in vitro on ER+ and ER− human breast tumor cell lines: MCF-7 and MDA-MD-231.

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ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.