Aromatase

Aminoglutethimide (BA-16038), an aromatase inhibitor, is used in the therapy of advanced BREAST Y.

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

Vorozole (R83842) is an orally active, potent, and selective nonsteroidal aromatase inhibitor.Vorozole exhibits antitumor activity in vivo and may be used in the study of breast cancer.

Anastrozole (ZD1033)(ZD1033), a potent and highly selective aromatase (CYP19) inhibitor (IC50 = 15 nM), has no obvious effect on adrenocorticoid hormone synthesis.

Finrozole (MPV 2213ad) is a novel selective aromatase inhibitor that is partially reversible for breast development.

(-)-Vorozole is an orally active non-steroidal aromatase inhibitor with potency and selectivity. (-)-Vorozole has demonstrated antitumor activity in in vivo experiments. (-)-Vorozole is used in the study of breast cancer.

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

(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.

Eriodictyol chalcone has anti-plasmodial effects on P. falciparum growth.

Minamestane is a novel irreversible aromatase inhibitor.Minamestane induces time-dependent inhibition of human placental aromatase with a half-life of 4 minutes and a K of 59 nM.Minamestane has antitumor activity.

LY 43578 is an orally active aromatase inhibitor. LY43578 could inhibit O-demethylation of P-450-dependent p-nitroanisole and N-demethylation of ethylmorphine (IC50 of 0.3 and 5 μm, respectively) in rat liver microsomes. LY 43578 can be used to study neurological and cardiovascular diseases.

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.

Fadrozole is a nonsteroidal aromatase inhibitor with potential antineoplastic activity(IC50 : 6.4 nM)

alpha-Naphthoflavone (7,8-benzoflavone), a synthetic flavonoid, is a potent inhibitor of aromatase with an I50 value of 0.5 μM.

Org30958 is a potent inhibitor of aromatase in vivo.

Calceolarioside B (Desrhamnosyl isoacteoside) displays inhibition of aromatase. Calceolarioside B displays inhibition of human recombinant PKCalpha.

Oleuropein is an antioxidant polyphenol isolated from olive leaf.

Flavanone (2-Phenylchroman-4-one)s from citrus fruits have also been shown to exert beneficial effects on human vascular function. In particular, chronic interventions with orange juice, or the pure flavanone hesperidin, resulted in a decrease in blood pressure in overweight volunteers and acute improvements in microvascular reactivity.

3-(3,4-Dimethoxyphenyl)propanoic acid (3,4-Dimethoxyhydrocinnamic acid) is an orally active short-chain fatty acid (SCFAs). It promotes γ-globin gene expression and erythropoiesis in vivo and can be used in beta hemoglobinopathies and other anemias.

Exemestane (EXE) is an Aromatase Inhibitor. The mechanism of action of exemestane is as an Aromatase Inhibitor.

Fadrozole hydrochloride (CGS 16949A) is a model aromatase inhibitor that has been shown to suppress estrogen production in the ovaries of fish.

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