title: Non-isomerisable antiestrogens related to tamoxifen.
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.
authors.affiliation: Drug Development Section, Institute of Cancer Research, Sutton, Surrey, England.
authors.forename: R
authors.initials: R
authors.lastname: McCague
authors.forename: M
authors.initials: M
authors.lastname: Jarman
authors.forename: O T
authors.initials: OT
authors.lastname: Leung
authors.forename: A B
authors.initials: AB
authors.lastname: Foster
authors.forename: G
authors.initials: G
authors.lastname: Leclercq
authors.forename: S
authors.initials: S
authors.lastname: Stoessel
mesh_terms: D000818:Animals; D001681:Biological Assay; D002455:Cell Division / Q000187:drug effects; D004965:Estrogen Antagonists / Q000378:metabolism; D006801:Humans; D007536:Isomerism; D011960:Receptors, Estrogen / Q000378:metabolism; D013329:Structure-Activity Relationship; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000378:metabolism
chemical_list: D004965:Estrogen Antagonists; D011960:Receptors, Estrogen; D013629:Tamoxifen