Synthesis of Androst-5-en-7-ones and Androsta-3,5-dien-7-ones and Their Related 7-Deoxy Analogs as Conformational and Catalytic Probes for the Active Site of Aromatase

A series of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their 7-deoxy derivatives, respectively, were synthesized and tested for their abilities to inhibit aromatase in human placental microsomes. All the steroids inhibited the enzyme in a competitive manner with Ki's ranging from 0.05...

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Veröffentlicht in:	Journal of medicinal chemistry 1994-07, Vol.37 (14), p.2198-2205
Hauptverfasser:	Numazawa, Mitsuteru, Mutsumi, Ayako, Tachibana, Mii, Hoshi, Kumiko
Format:	Artikel
Sprache:	eng
Schlagworte:	Androstadienes - chemical synthesis Androstadienes - pharmacology Androstenes - chemical synthesis Androstenes - pharmacology Antineoplastic agents Aromatase Inhibitors Binding Sites Biological and medical sciences General aspects Humans Kinetics Medical sciences Molecular Conformation Pharmacology. Drug treatments Structure-Activity Relationship
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