Non-isomerisable antiestrogens related to tamoxifen.
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.
McCague
R
R
Drug Development Section, Institute of Cancer Research, Sutton, Surrey, England.
Jarman
M
M
Leung
O T
OT
Foster
A B
AB
Leclercq
G
G
Stoessel
S
S
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
D004965:Estrogen Antagonists; D011960:Receptors, Estrogen; D013629:Tamoxifen