Article révisé par les pairs
Résumé : Three types of non-isomerisable antiestrogens analogous to tamoxifen and 4-hydroxy-tamoxifen 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. © 1988.