Synthesis and Biological Evaluation of Spiro--lactones as Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 2 (17β-HSD2)

…, S Marchais-Oberwinkler

文献索引：Xu, Kuiying; Wetzel, Marie; Hartmann, Rolf W.; Marchais-Oberwinkler, Sandrine Letters in Drug Design and Discovery, 2011 , vol. 8, # 5 p. 406 - 421

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被引用次数: 9

摘要

17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyzes the oxidation of the potent estradiol (E2) to the less active estrogen estrone (E1). Inhibitors of this enzyme should maintain the local level of E2 in bone tissue when the E2 concentration in the circulation drops and therefore might be useful for the treatment of osteoporosis. In this work, novel non- steroidal spiro--lactone compounds designed as 17β-HSD2 inhibitors were synthesized ...