22393-62-0_peak 2 exhibits some aspects of the antiestrogenic activity and other actions that may be connected to the estrogenic properties. A mixture of the (Z)- and (E)-isomers (Broparestrol, INN) is used in dermatology.
N-Desmethyltamoxifen, the principal metabolite of tamoxifen in humans, serves as an efficacious modulator of ceramide metabolism within human AML cells by inhibiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation. Although it demonstrates weak antiestrogenic properties, it acts as a protein kinase C (PKC) inhibitor with a potency ten times greater than that of tamoxifen.
Zuclomiphene citrate is a cis isomer of Clomiphene citrate, and has an antiestrogenic effect and can inhibit the secretion of luteinizing hormone (LH) more than the trans isomer.
Arzoxifene (LY353381) is an orally active selective estrogen receptor modulator (SERM) exhibiting a fixed ring structure analogous to raloxifene. This compound demonstrates potent antiestrogenic effects on breast cancer and endometrium while displaying minimal side effects. Additionally, Arzoxifene elicits favorable estrogenic effects on bone health and lipid profile.
TAS-108, also known as SR16234, is a synthetic, antiestrogenic steroidal compound with potential antitumor activity. TAS-108 binds to and inhibits estrogenic receptor alpha (ERa), mainly expressed in the mammary gland and uterus and upregulated in estrogen-dependent tumors. Blockage of ERa by TAS-108 prevents the binding and effects of estrogen and may lead to an inhibition of estrogen-dependent cancer cell proliferation. TAS-108 also is a partial agonist of the estrogenic receptor beta (ERb), expressed in many tissues including the central nervous system, urogenital tract, bone and cardiovascular system, thereby exerting a positive effect on these tissues.
Pachyaximine A possesses significant antibacterial activity against Escherichia coli, Staphylococcus aureus, Corynebacterium diphtheriae and Corynebacterium pyrogenes. (-)-Pachyaximine A demonstrates significant activity as antiestrogen binding site (AEBS