Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.

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Browne LJ, Gude C, Rodriguez H, Steele RE, Bhatnager A

Fadrozole hydrochloride: a potent, selective, nonsteroidal inhibitor of aromatase for the treatment of estrogen-dependent disease.

J Med Chem. 1991 Feb;34(2):725-36.

PubMed ID
1825337 [ View in PubMed
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Abstract

A new class of potent, selective, nonsteroidal inhibitors of aromatase have been discovered. The most potent member of this series is fadrozole hydrochloride, CGS 16949 A, 4-(5,6,7,8-tetrahydroimidazo[1,5-alpha]pyridin-5-yl)benzonitrile monohydrochloride, 26a. In addition, the 6,7-dihydropyrrolo[1,2-c]imidazole (21a) and the 6,7,8,9-tetrahydroimidazo[1,5-alpha]azepine (21b) analogues were synthesized and evaluated. CGS 16949 A's ability to selectively inhibit aromatase (IC50 = 4.5 nM) over other cytochrome P-450 enzymes and suppress estrogen production when administered orally make it a suitable candidate to test the potential of an aromatase inhibitor in estrogen-dependent diseases including breast cancer.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
AminoglutethimideCholesterol side-chain cleavage enzyme, mitochondrialIC 50 (nM)80000N/AN/ADetails
AminoglutethimideCytochrome P450 19A1IC 50 (nM)1700N/AN/ADetails
AminoglutethimideCytochrome P450 19A1Ki (nM)470N/AN/ADetails
AminoglutethimideCytochrome P450 19A1IC 50 (nM)30000N/AN/ADetails