aromatase,estrogen

Prochloraz (Prelude) 是咪唑类抗真菌剂。Prochloraz 抑制羊毛甾醇的细胞色素 P450 依赖性 14α-脱甲基作用，由此抑制麦角固醇的生物合成，从而导致真菌细胞膜破裂和细胞死亡。它也是雌激素受体和 雄激素受体的拮抗剂，IC50分别为25 μM 和4 μM， 并激活芳烃受体，EC50为1μM。

Endoxifen hydrochloride，Tamoxifen的主要活性代谢产物，具备较高的对雌激素受体(estrogen receptor)的亲和力和特异性，并能抑制芳香酶活性。它在乳腺癌研究中表现出潜在应用价值。

Letrozole (CGS 20267) 是一种可口服的，选择性可逆的非甾体类芳香化酶抑制剂，IC50值为 11.5 nM。它选择性抑制雌激素的生物合成，可研究乳腺癌。

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) 是一种咪唑衍生物，是一种具有口服活性的维甲酸 (RA) 代谢阻断剂(RAMBA)，具有抗肿瘤作用。它能够抑制维甲酸依赖的细胞色素P450(CYP26) 4- 羟基化 (IC50=7 μM)，导致组织维甲酸水平增加。

(S)-Dexfadrostat ((S)-Fadrozole) 作为一种芳香化酶抑制剂，其IC50值仅为 4.6 nM，能够有效抑制人胎盘微粒体中的芳香化酶活性。该化合物主要用于研究雌激素依赖性乳腺癌、男性乳房发育症以及系统性红斑狼疮。

S-(-)-Aminoglutethimide D-tartrate为一种控制某些癌症类型的芳香化酶抑制剂，其作用机制是通过抑制酶活性，有效降低睾酮和雌激素水平，从而阻断肾上腺类固醇的生成。此化合物还可用于治疗与类固醇相关的疾病。

Fadrozole是一种选择性芳香酶抑制剂，有效用于治疗依赖雌性激素的疾病，包括乳腺癌。

Aromatase-IN-4 (Compound 6a) 是一种芳香酶 (Aromatase) 抑制剂，具有抗癌活性。其对 MDAMB-231、MCF-7、A-549、NCI-H23 和 A-498 细胞系的GI50值分别为 2.95 μM、3.35 μM、2.27 μM、8.46 nM 和 1.56 μM。Aromatase-IN-4 能有效阻止芳香酶依赖的雌激素生成。

Endoxifen Z-isomer (EDX)是 Tamoxifen 重要的代谢产物,在表达 ERα的乳腺癌细胞中发挥抗雌激素作用。它以浓度依赖的方式抑制 hERG, IC50值为1.6μM。

YM 511 是一种高度特异性的非甾体芳香酶 (aromatase) 抑制剂。YM 511 竞争性抑制大鼠卵巢和人胎盘微粒体中的芳香酶活性 (IC50 分别为 0.4 和 0.12 nM)。YM 511 轻微抑制其他类固醇激素的产生。YM 511 具有用于抑制雌激素依赖性作用研究，不会影响其他类固醇激素的血清水平的潜力。

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

Obacunone 是从沼泽白葡萄柚种子中分离得到的，通过诱导凋亡发挥抗癌作用。它在雄激素依赖性人前列腺 Y 细胞中具有细胞毒性。它对鼠伤寒沙门氏菌具有抗毒作用，可作为开发鼠伤寒沙门氏菌抗毒策略的先导化合物。

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.

Endoxifen ((E Z)-Endoxifen) 是 Tamoxifen 的关键活性代谢物，能抑制芳香酶的活性，与雌激素受体有较高的亲和力和特异性。它有潜力研究乳腺癌。

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) 是一种选择性的、有效，和非甾体类的芳香化酶抑制剂(IC50:6.4 nM)。

10-Chloroestra-1,4-diene-3,17-dione 是一个对雌性激素受体α (ERα) 具有激动作用的类固醇。它能增加在S. cerevisiae 中报告基因的表达（对人类受体的EC50 = 0.36 nM）。同时，它也是一种芳香化酶抑制剂（IC50 = 2.4 µM）。