ChemInform Abstract: Fadrozole Hydrochloride: A Potent, Selective, Nonsteroidal Inhibitor of Aromatase for the Treatment of Estrogen-Dependent Disease

Autor:	Hermann Rodriguez, A. Bhatnager, L. J. Browne, Steele Ronald Edward, Candido Gude
Rok vydání:	2010
Předmět:	chemistry.chemical_classification Aromatase inhibitor Nonsteroidal biology Cytochrome medicine.drug_class General Medicine Pharmacology chemistry.chemical_compound Enzyme chemistry Biochemistry Estrogen medicine biology.protein Aromatase Azepine IC50
Zdroj:	ChemInform. 22
ISSN:	0931-7597
DOI:	10.1002/chin.199139167
Popis:	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.
Databáze:	OpenAIRE
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