Laboratory of Medicinal Chemistry, CHUQ - Research Center and Laval University, 2705 Laurier Blvd., Québec, Canada G1V 4G2.
Bioorg Med Chem Lett. 2011 Sep 15;21(18):5510-3. doi: 10.1016/j.bmcl.2011.06.110. Epub 2011 Jun 30.
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.
基于经过修饰的 3-羟基-雌甾-1,3,5(10)-三烯核心结构，设计了一种非雌激素的 17β-羟甾脱氢酶 1 型（17β-HSD1）抑制剂，该核心结构具有额外的五元内酯环和苯甲酰胺基团。合成了该抑制剂，对其进行了全面的表征，并测试了其抑制酶活性的能力。还研究了其雌激素活性，并在雌激素依赖性 T-47D 细胞系上进行了测试。有趣的是，这种甾体衍生物对 17β-HSD1 具有抑制作用，且没有残留的非预期雌激素活性。
