antiestrogen

N-Desmethyltamoxifen hydrochloride is the primary metabolite of tamoxifen in humans.

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.

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.

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.

EM-651 (2H-1-Benzopyran-7-ol, 3-(4-hydroxyphenyl)-4-methyl-2-[4-[2-(1-piperidinyl)ethoxy]phenyl]-, (2R)-) is an enantiomer of EM-652, IC50=20.0 nM. EM-652 is an orally active pure antiestrogen and selective estrogen receptor antagonist, IC50=0.44nM.

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

GW7604 is an antiestrogen and it also is the metabolite of GW5638. GW5638 is an antagonist of high-affinity estrogen receptor (ER).

PBPE hydrochloride is a derivative of tamoxifen and functions as a selective ligand for antiestrogen binding sites (AEBS). The binding affinity (Ki) of PBPE hydrochloride and MBPE to AEBS is 8.79 nM and 17.57 nM, respectively.

Pure antiestrogen that downregulates estrogen receptor expression

Anordiol is an antiestrogen with estrogenic activity. It also is known to inhibit fertility.

Clometherone is a synthetic pregnane steroid and derivative of progesterone which is used as an antiestrogen and antiandrogen.

Trioxifene mesylate is an antiestrogen that suppresses growth hormone secretion.

Bexirestrant is an orally active ER-α degrader commonly employed in antiestrogen and antineoplastic therapy research.

Pipendoxifene, also known as ERA-923, is a new antiestrogen with potential anticancer activity. ERA-923 potently inhibits estrogen binding to ER-alpha (IC50 = 14 nM). In ER-alpha-positive human MCF-7 breast carcinoma cells, ERA-923 inhibits estrogen-stimulated growth (IC50 = 0.2 nM) associated with cytostasis. In vitro, a MCF-7 variant with inherent resistance to tamoxifen (10-fold) or 4-OH tamoxifen (>1000-fold) retains complete sensitivity to ERA-923 . In preclinical models, ERA-923 has an improved efficacy and safety compared with tamoxifen. In the combination with temsirolimus, ERA-923 showed excellent anticancer activity in preclinical models.

Axillaridine A is a new cholinesterase inhibitors, it may act as potential leads in the discovery of clinically useful inhibitors for nervous-system disorders, particularly by reducing memory deficiency in Alzheimer's disease patients by potentiating and

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