Cytotoxicity and Antiestrogenicity of a Novel Series of Basic Diphenylethylenes
- 1 March 1997
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 40 (7) , 1104-1111
- https://doi.org/10.1021/jm950624t
Abstract
On the premise that it is necessary to develop antiestrogens with a higher cytotoxic component in order to reduce the risks of the development of heterogeneous malignant cell populations in breast cancer, we studied a novel series of basic diphenylethylenes, for the most part devoid of estrogenic activity, with low antiestrogenicity but much enhanced cytotoxicity compared to the reference drug tamoxifen. The main structural features associated with cytotoxicity were E isomery, substituents of five to eight carbons on the ethylene bond, and dibasicity.Keywords
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