aromatase,estrogen

Prochloraz (Prelude) is a broad-spectrum contact imidazole fungicide. Prochloraz inhibits human placental microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an estrogen receptor (IC50s = 25 μM) and androgen receptor (IC50 = 4 μM) antagonist, and activates aryl hydrocarbon receptors (EC50 = 1 μM).

Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor (Ki: 0.18 μM) that inhibits estrogen biosynthesis, exhibits antifertility effects, and induces impairment of spatial memory.

Endoxifen hydrochloride, a principal active metabolite of Tamoxifen (TAM), exhibits heightened affinity and specificity towards the estrogen receptor and possesses aromatase inhibitory capability. It holds promise for breast cancer research.

Letrozole (CGS 20267) is an Aromatase Inhibitor. The mechanism of action of letrozole is as an Aromatase Inhibitor.

Liarozole dihydrochloride is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.

Liarozole (R75251 dihydrochloride) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase).Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.

(S)-Dexfadrostat ((S)-Fadrozole), an aromatase inhibitor, exhibits an IC 50 of 4.6 nM in in vitro assays using human placental microsomes. It is applicable for research on estrogen-dependent breast cancer, gynecomastia, and systemic lupus erythematosus.

S-(-)-Aminoglutethimide D-tartrate serves as an aromatase inhibitor that possesses the capacity to obstruct adrenal steroid production. It is commonly employed clinically to manage certain types of cancer and is utilized in targeting diseases associated with steroids. By inhibiting enzyme activity, S-(-)-Aminoglutethimide D-tartrate effectively reduces levels of testosterone and estrogen.

Fadrozole is a selective aromatase inhibitor used effectively in the treatment of estrogen-dependent conditions, such as breast cancer.

Aromatase-IN-4 (Compound 6a) is an inhibitor of the enzyme aromatase. It displays anticancer properties, with GI50 values for different cell lines as follows: 2.95 μM for MDAMB-231, 3.35 μM for MCF-7, 2.27 μM for A-549, 8.46 nM for NCI-H23, and 1.56 μM for A-498. Aromatase-IN-4 effectively blocks the estrogen production that depends on aromatase.

Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. It effectively blocks estrogen production and inhibits the proliferation of breast cancer cell lines such as MCF-7, arresting the cell cycle in the G1 phase and inducing apoptosis. Aromatase-IN-5 shows promise for breast cancer research.

Aromatase-IN-3 (compound 7d) is an aromatase inhibitor with an IC50 of 54 nM. It effectively suppresses the conversion of androstenedione to estrogen catalyzed by aromatase, demonstrating significant tumor growth inhibition in breast cancer cell lines, suggesting its potential application in ER+ cancer research.

PROTACERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader designed to diminish estrogen receptor α (ERα) and aromatase (ARO). It demonstrates a Ki of 0.25 μM for ERα binding and an IC50 of 4.6 μM for ARO inhibition. This compound curbs proliferation in wild-type MCF-7 cells (IC50=0.54 μM) and ERα mutant variants MCF-7EGFR (IC50=0.075 μM), MCF-7D538G (IC50=0.31 μM), and MCF-7Y537S (IC50=2.3 μM), while also downregulating ERS1 and MYC expression. PROTACERα Degrader-9 arrests the cell cycle at the G2/M phase and induces apoptosis in MCF-7 cells, exhibiting antitumor efficacy in mouse models.

ERα degrader9 is a dual-targeting ligand designed for the estrogen receptor α (ERα) and aromatase (ARO). It can be utilized in the synthesis of PROTACERαDegrader-9.

Endoxifen Z-isomer (EDX) is a key active metabolite of tamoxifen (TAM) with higher affinity and specificity to estrogen receptors that also inhibits aromatase activity.

YM 511 is a highly specific non-steroidal aromatase inhibitor. YM 511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM 511 slightly inhibits production of other steroid hormones. YM 511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones.

LY 113174, a novel nonsteroidal aromatase inhibitor, may prove useful in the treatment of estrogen-dependent diseases.

Obacunone has cytotoxicity in androgen-dependent human prostate Y cells. Obacunone exerts an antivirulence effect on S. Typhimurium and may serve as a lead compound for development of antivirulence strategies for S. Typhimurium. Obacunone may have the pot

17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.

(E/Z)-Endoxifen ((E/Z)-Endoxifen) is an active metabolite of tamoxifen produced by the sequential action of cytochrome P450 (CYP) isoforms, including CYP2D6. It is a strong anti-estrogen, as it has an approximately 100-fold greater affinity for estrogen receptors than tamoxifen. As the efficient conversion of tamoxifen to endoxifen depends on CYP2D6, polymorphisms in this CYP isoform can impact the effectiveness of TMX treatment.

Norendoxifen, also known as 4-hydroxy-N, N-didesmethyltamoxifen, is a nonsteroidal aromatase inhibitor of the triphenylethylene group that was never marketed. It is an active metabolite of the selective estrogen receptor modulator tamoxifen.

Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders. Endoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group. It is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce afimoxifene (4-hydroxytamoxifen) and endoxifen.

Fadrozole is a selective inhibitor of aromatase. It also effective in the treatment of estrogen-dependent diseases including breast cancer.

Fadrozole hydrochloride (CGS 16949A) is a model aromatase inhibitor that effectively suppresses estrogen production in fish ovaries.