Synthesis of substituted 15β-alkoxy estrone derivatives and their cofactor-dependent inhibitory effect on 17β-HSD1

17β-Hydroxysteroid dehydrogenase type 1 (17β-HSD1) is a key enzyme in the biosynthesis of 17β-estradiol. Novel estrone-based compounds bearing various 15β-oxa-linked substituents and hydroxy, methoxy, benzyloxy, and sulfamate groups in position C3 as potential 17β-HSD1 inhibitors have been synthesiz...

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Veröffentlicht in:	Journal of enzyme inhibition and medicinal chemistry 2019-01, Vol.34 (1), p.1271-1286
Hauptverfasser:	Herman, Bianka Edina, Kiss, Anita, Wölfling, János, Mernyák, Erzsébet, Szécsi, Mihály, Schneider, Gyula
Format:	Artikel
Sprache:	eng
Schlagworte:	17-Hydroxysteroid Dehydrogenases - antagonists & inhibitors 17-Hydroxysteroid Dehydrogenases - metabolism 17β-HSD1 Dose-Response Relationship, Drug Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacology estrogen biosynthesis Estrone - chemical synthesis Estrone - chemistry Estrone - pharmacology Humans Michael addition Molecular Conformation NADPH and NADH Research Paper Structure-Activity Relationship substituted 15β-alkoxy-estrone derivatives
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