Chlorotrianisene (tri-p-anisylchloroethylene) is an orally bioavailable, highly lipophilic, synthetic triphenylethylene (TPE) derivative and selective estrogen receptor modulator (SERM), with predominantly estrogenic but also antiestrogenic activities.

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.

FLTX1 is a fluorescent derivative of Tamoxifen, designed to efficiently target and label intracellular Tamoxifen-binding sites (estrogen receptors) both under permeabilized and non-permeabilized conditions. Additionally, FLTX1 demonstrates strong antiestrogenic activity in breast cancer cells, resembling the potent antiestrogenic properties of Tamoxifen. Notably, FLTX1 does not exhibit any estrogenic agonistic effect on the uterus.

LY 183648 has antiestrogenic activity. LY117018 inhibited PAIII metastasis to the gluteal (97%) and iliac lymph nodes (88%).

Millewanin G shows antiestrogenic activity.

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.

Endoxifen E-isomer (E-Endoxifen) is the E-isomer of (Z)-Endoxifen. Endoxifen E-isomer has antiestrogenic effects.

RU 45144 is an estradiol derivative with antiestrogenic activity.

HIF-1α-IN-3, also known as Compound (S)-3f, is a hypoxia-selective inhibitor of HIF-1α. It exhibits potent antiestrogenic activity [1].

Millewanins H shows antiestrogenic activity.

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

Tracheloside significantly decreases the activity of alkaline phosphatase (IC50: 0.31 μg/ml), a level of inhibition comparable to that of tamoxifen (IC50: 0.43 μg/ml).

7-Hydroxyflavanone shows antimicrobial activity against Streptococcus pneumoniae clinical isolates.

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.

OP-1074 is a pure antiestrogen and a selective degrader of ER, shows specific antiestrogenic activity for ERα and ERβ.