| S1235 |
Letrozole
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Letrozole is a third generation inhibitor of aromatase with IC50 of 0.07-20 nM in cell-free assays. It has no effect on the plasma levels of 17α-OH progesterone, thyroid-stimulating hormone (TSH), luteinizing hormone (LH), follicle-stimulating hormone (FSH), or androstenedione and does not affect normal urine electrolyte excretion or thyroid function in clinical studies. This compound induces autophagy.
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Mol Syst Biol, 2025, 10.1038/s44320-025-00104-6
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Exp Neurol, 2025, 392:115365
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eNeuro, 2024, 11(8)ENEURO.0332-24.2024
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| S1188 |
Anastrozole
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Anastrozole is a third-generation nonsteroidal selective aromatase inhibitor. It may offer greater selectivity compared with other aromatase inhibitors, being without any intrinsic endocrine effects and with no apparent effect on the synthesis of adrenal steroids.
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Mol Oncol, 2023, 10.1002/1878-0261.13541
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Commun Biol, 2023, 6(1):695
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Cell Discov, 2022, 8(1):40
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| S1196 |
Exemestane
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Exemestane is an aromatase inhibitor, inhibits human placental and rat ovarian aromatase with IC50 of 30 nM and 40 nM, respectively.
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Commun Biol, 2023, 6(1):695
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Front Mol Biosci, 2022, 9:981962
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J Pers Med, 2022, 12(2)258
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| S3784 |
Obacunone (AI3-37934)
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Obacunone (AI3-37934, CCRIS 8657), a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. This compound significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; it is also a novel activator of Nrf2.
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Int J Mol Sci, 2023, 24(14)11484
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University of Valencia, 2023,
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Cell Mol Biol Lett, 2022, 27(1):29
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| S9519 |
Fadrozole (CGS16949A)
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Fadrozole (CGS16949A) is a potent, selective, nonsteroidal inhibitor of aromatase with an IC50 of 4.5 nM and selectivity over other cytochrome P-450 enzymes.
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iScience, 2024, 27(10):110862
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Epigenetics Chromatin, 2023, 16(1):2
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Drug Test Anal, 2020, 10.1002/dta.2917
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| S5158 |
alpha-Naphthoflavone
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Alpha-Naphthoflavone (7,8-benzoflavone), a synthetic flavonoid, is a potent inhibitor of aromatase with an I50 value of 0.5 μM.
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| S7867 |
Oleuropein
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Oleuropein is an antioxidant polyphenol isolated from olive leaf. It exerts antioxidant, anti-inflammatory and anti-atherogenic effects and suppresses the adipocyte differentiation in vitro. This compound inhibits PPARγ activity. It exerts anti-adipogenic effect through direct inhibition of PPARγ transcriptional activity. This chemical also inhibits aromatase. It induces apoptosis. Phase 2.
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Front Endocrinol (Lausanne), 2024, 15:1354435
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J Med Virol, 2019, 91(8):1440-1447
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