Structure-based design, synthesis and in vitro characterization of potent 17β-hydroxysteroid dehydrogenase type 1 inhibitors based on 2-substitutions of estrone and D-homo-estrone

Bioorganic & Medicinal Chemistry Letters(2009)

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摘要
The development of 17β-HSD1 inhibitor (e.g., 2-phenethyl-D-homo-estrone with IC50 of 15nM in vitro) is reported.
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关键词
Steroid metabolism,Cancer,Inhibitors,Molecular docking,Structure-based drug design
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