A time-dependent inactivation of aromatase by 19-substituted androst-4-ene-3,6,17-triones

Diastereomeric (19S)- and (19R)-19-ethynyl-19-acetoxy derivatives of androst-4-ene-3,6,17-trione (AT) (9 and 10) and 19,19-difluoro AT ( 12) were synthesized. The 19,19-difluoro compound ( 12) was an effective competitive inhibitor of human placental aromatase with an inhibition constant (k:) of 1.8...

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Veröffentlicht in:	Steroids 1993, Vol.58 (1), p.40-46
Hauptverfasser:	Mitsuteru, Numazawa, Ayako, Mutsumi, Naomi, Asano, Yuri, Ito
Format:	Artikel
Sprache:	eng
Schlagworte:	19,19-difluoroandrost-4-ene-3,6,17-trione 19-ethynyl-19-acetoxyandrost-4-ene-3,6,17-trione Analytical, structural and metabolic biochemistry Androstenes - chemical synthesis Androstenes - chemistry Androstenes - pharmacology aromatase Aromatase Inhibitors Binding, Competitive Biological and medical sciences chemical synthesis Female Fundamental and applied biological sciences. Psychology Humans Kinetics Magnetic Resonance Spectroscopy Microsomes - enzymology NADP - pharmacology Other biological molecules Placenta - enzymology Placenta - ultrastructure Stereoisomerism suicide substrate Terpenes, steroids. Hormones time-dependent inactivation
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