Ngatcha B T, Luu-The V, Poirier D
Medicinal Chemistry Division, Oncology and Molecular Endocrinology Research Center, Laval University Medical Center (CHUL) and Laval University, Quebec, Canada.
Bioorg Med Chem Lett. 2000 Nov 20;10(22):2533-6. doi: 10.1016/s0960-894x(00)00517-5.
Androsterone derivatives substituted at position 3 were synthesized starting from dihydrotestosterone in a short sequence of reactions. They proved to be potent inhibitors (IC50 = 57-147 nM) of type 3 17beta-hydroxysteroid dehydrogenase, a key enzyme of steroidogenesis, which catalyzes the transformation of androstenedione to steroid active androgen testosterone.
以双氢睾酮为起始原料，通过短反应序列合成了在3位被取代的雄甾酮衍生物。它们被证明是3型17β-羟基类固醇脱氢酶的有效抑制剂（IC50 = 57 - 147 nM），3型17β-羟基类固醇脱氢酶是类固醇生成的关键酶，催化雄烯二酮转化为具有活性的雄激素睾酮。
