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Non-isomerisable antiestrogens related to tamoxifen
R McCague1, M Jarman, O T Leung
1Drug Development Section, Institute of Cancer Research, Sutton, Surrey, England.
Abstract:
Three types of non-isomerisable antiestrogens analogous to tamoxifen and 4-hydroxytamoxifen are described. Advantages of non-isomerisability are simplified synthesis, simplified metabolism profile, and that structure-activity relationships become more meaningful. The compounds described differ from tamoxifen by having an extra ring methyl group, a fused seven-membered ring system, or the central ethylene linkage saturated. These compounds retained both binding affinity to estrogen receptors and growth inhibition of MCF-7 human breast cancer cells in vitro.
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