Non-isomerisable antiestrogens related to tamoxifen

McCague, Raymond; Jarman, Michael; Leung, On-Tai; Foster, Allan A.B.; Leclercq, Guy; Stoessel, Susanna

doi:doi/10.1016/0022-4731(88)90005-2

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Non-isomerisable antiestrogens related to tamoxifen

par McCague, Raymond ;Jarman, Michael ;Leung, On-Tai ;Foster, Allan A.B.;Leclercq, Guy

;Stoessel, Susanna
Référence Journal of Steroid Biochemistry, 31, 4, page (545-547)
Publication Publié, 1988

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.

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