Synthesis and preliminary evaluation of a modified estradiol-core bearing a fused γ-lactone as non-estrogenic inhibitor of 17β-hydroxysteroid dehydrogenase type 1

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• 作者：É ; tienne Ouellet^a ; Diana Ayan^a ; Donald Poirier ; ^a ; ^{donald.poirier@crchul.ulaval.ca"" rel=""nofollow}
• 关键词：17&#x3b2 ; -Hydroxysteroid dehydrogenase ; Steroid ; Estradiol ; Inhibitor ; Enzyme ; Breast cancer
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2011
• 出版时间：15 September 2011
• 年：2011
• 卷：21
• 期：18
• 页码：5510-5513
• 全文大小：380 K

文摘

A non-estrogenic inhibitor of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) was designed based on a modified 3-hydroxy-estra-1,3,5(10)-triene core having an additional five-member lactone ring and a benzamide group. The inhibitor was synthesized, fully characterized and tested for its ability to inhibit the enzyme activity. Estrogenicity was also investigated and tested on estrogen-dependent T-47D cell line. Interestingly, this steroid derivative showed inhibitory potency towards 17β-HSD1 and did not present residual unwanted estrogenic activity.