Journal of medicinal chemistry

Synthesis and optimization of a new family of type 3 17β-hydroxysteroid dehydrogenase inhibitors by parallel liquid-phase chemistry

R Maltais, V Luu-The, D Poirier

文献索引：Maltais, Rene; Luu-The, Van; Poirier, Donald Journal of Medicinal Chemistry, 2002 , vol. 45, # 3 p. 640 - 653

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被引用次数: 57

摘要

Type 3 17β-hydroxysteroid dehydrogenase (17β-HSD) transforms 4-androstene-3, 17-dione (Δ4-dione) into the androgen testosterone. To produce potent inhibitors of this key steroidogenic enzyme, we performed parallel liquid-phase synthesis of 3β-substituted androsterone (ADT) libraries (AD) in good yields and average high-performance liquid chromatography (HPLC) purities of 92-94%. The first library (A) of 3β-amidomethyl-ADT ...