Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes.
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.
Gilbert
J
J
CNRS-SIRCOB, Université de Versailles/St. Quentin-en-Yvelines, France.
Fuentes
M
M
Ojasoo
T
T
Doré
J C
JC
Pons
M
M
D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology*; D002455:Cell Division / Q000187:drug effects; D018360:Crystallography, X-Ray; D004965:Estrogen Antagonists / Q000737:chemistry / Q000494:pharmacology*; D005030:Ethylenes / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015999:Multivariate Analysis; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D004965:Estrogen Antagonists; D005030:Ethylenes