CYTOTOXICITY AND ANTIESTROGENICITY OF A NOVEL SERIES OF BASIC DIPHENYLETHYLENES

On the premise that it is necessary to develop antiestrogens with a hi gher cytotoxic component in order to reduce the risks of the developme nt of heterogeneous malignant cell populations in breast cancer, we st udied a novel series of basic diphenylethylenes, for the most part dev oid of estrogenic activity, with low antiestrogenicity but much enhanc ed cytotoxicity compared to the reference drug tamoxifen. The main str uctural features associated with cytotoxicity were E isomery, substitu ents of five to eight carbons on the ethylene bond, and dibasicity.