Cytotoxicity and antiestrogenicity of a novel series of basic diphenylethylenes

Journal of Medicinal Chemistry
J GilbertM Pons


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.


Dec 3, 1990·Molecular and Cellular Endocrinology·L C Murphy
Dec 20, 1990·The Journal of Steroid Biochemistry and Molecular Biology·P D Darbre, R J Daly
Jan 1, 1987·Journal of Steroid Biochemistry·R L SutherlandP C Ruenitz
May 1, 1984·Molecular and Cellular Endocrinology·S BardonH Rochefort
Jun 1, 1995·Steroids·T OjasooJ C Doré
Jan 1, 1993·Breast Cancer Research and Treatment·K B Horwitz
Sep 1, 1993·The Journal of Steroid Biochemistry and Molecular Biology·E DemirpenceM Pons

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Feb 13, 2001·The Journal of Steroid Biochemistry and Molecular Biology·D HansJ C Doré
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Apr 28, 2006·Bioorganicheskaia khimiia·L E GolubovskaiaV M Rzheznikov
Dec 26, 2001·Chemical Reviews·H GaoC Hansch

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