J. Gilbert et al., CYTOTOXICITY AND ANTIESTROGENICITY OF A NOVEL SERIES OF BASIC DIPHENYLETHYLENES, Journal of medicinal chemistry, 40(7), 1997, pp. 1104-1111
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.