[Pyridyl-substituted tetralone derivatives: a new class of nonsteroidal aromatase inhibitors].
Structural modification of flavone and flavanone, two weak inhibitors of aromatase, led to the new compounds 1-7, the syntheses of which are described as well as the evaluation of their aromatase and desmolase inhibitory potency. With the exception of 2 all compounds show a stronger inhibition of aromatase than the parent compounds and are more effective inhibitors than aminoglutethimide (AG), the only commercially available compound. In contrast to AG compounds 1 and 3-7 exhibit no desmolase inhibitory activity. In case of AG this effect leads to undesirable side effects.
Bayer
H
H
Fachrichtung Pharmazeutische Chemie, Universität des Saarlandes.
Hartmann
R W
RW
D047072:Aromatase Inhibitors; D002786:Cholesterol Side-Chain Cleavage Enzyme / Q000037:antagonists & inhibitors; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D013764:Tetrahydronaphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology
D047072:Aromatase Inhibitors; D011725:Pyridines; D013764:Tetrahydronaphthalenes; D002786:Cholesterol Side-Chain Cleavage Enzyme
Pyridyl-substituierte Tetralonderivate: Eine neue Klasse nichtsteroidaler Aromatase-Inhibitoren.