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 ac...

Full description

Saved in:
Bibliographic Details
Published in:Journal of medicinal chemistry 1997-03, Vol.40 (7), p.1104-1111
Main Authors: Gilbert, Jacques, Fuentes, Maryse, Ojasoo, Tiiu, Doré, Jean-Christophe, Pons, Michel
Format: Article
Language:English
Subjects:
Antineoplastic agents
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Biological and medical sciences
Cell Division - drug effects
Crystallography, X-Ray
Estrogen Antagonists - chemistry
Estrogen Antagonists - pharmacology
Ethylenes - chemistry
Ethylenes - pharmacology
General aspects
Humans
Magnetic Resonance Spectroscopy
Mass Spectrometry
Medical sciences
Multivariate Analysis
Pharmacology. Drug treatments
Tumor Cells, Cultured
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm950624t