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...

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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
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cited_by cdi_FETCH-LOGICAL-a408t-6948f545c09d68d8f6388e7542de222918851f1898c0a98c112f7f059ad4363c3
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container_end_page 1111
container_issue 7
container_start_page 1104
container_title Journal of medicinal chemistry
container_volume 40
creator Gilbert, Jacques
Fuentes, Maryse
Ojasoo, Tiiu
Doré, Jean-Christophe
Pons, Michel
description 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.
doi_str_mv 10.1021/jm950624t
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source American Chemical Society:Jisc Collections:American Chemical Society Read & Publish Agreement 2022-2024 (Reading list)
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
title Cytotoxicity and Antiestrogenicity of a Novel Series of Basic Diphenylethylenes
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