Inhibition of 17β-HSD1: SAR of bicyclic substituted hydroxyphenylmethanones and discovery of new potent inhibitors with thioether linker

AS Abdelsamie, E Bey, N Hanke, M Empting…

文献索引：Abdelsamie, Ahmed S.; Bey, Emmanuel; Hanke, Nina; Empting, Martin; Hartmann, Rolf W.; Frotscher, Martin European Journal of Medicinal Chemistry, 2014 , vol. 82, p. 394 - 406

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被引用次数: 4

摘要

Abstract Estradiol is the most potent estrogen in humans. It is known to be involved in the development and proliferation of estrogen dependent diseases such as breast cancer and endometriosis. The last step of its biosynthesis is catalyzed by 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) which consequently is a promising target for the treatment of these diseases. Recently, we reported on bicyclic substituted ...