Estrogen receptor-binding affinity of tamoxifen analogs with various side chains and their biologic profile in immature rat uterus.
Estrogen receptor-binding affinity and estrogenic and antiestrogenic activity have been evaluated for tamoxifen analogs substituted with various side chains. Antagonist activity of the compounds of this series appears to be dependent on the presence of the beta-tert-aminoethoxy moiety. The results also indicate that the dissociation of these compounds from the estrogen receptor-binding site at 25 C is very slow.
Agarwal
A K
AK
Division of Endocrinology, Central Drug Research Institute, Lucknow, India.
Bindal
R D
RD
D000818:Animals; D005260:Female; D066298:In Vitro Techniques; D051381:Rats; D011919:Rats, Inbred Strains; D011960:Receptors, Estrogen / Q000187:drug effects*; D013629:Tamoxifen / Q000031:analogs & derivatives* / Q000494:pharmacology; D014599:Uterus / Q000187:drug effects*
D011960:Receptors, Estrogen; D013629:Tamoxifen