Penov Gasi Katarina M, Miljković Dusan A, Medić Mijacević Ljubica D, Djurendić Evgenija A, Stojanović Srdjan Z, Sakac Marija N, Djurendić Maja Dj, Stanković Slobodanka M, Lazar Dusan, Andrić Silvana, Kovacević Radmila
Department of Chemistry, Faculty of Sciences, University of Novi Sad, 21000 Novi Sad, Trg Dositeja Obradovića 3, Serbia and Montenegro, Yugoslavia.
Steroids. 2003 Sep;68(7-8):667-76. doi: 10.1016/s0039-128x(03)00097-7.
D-Homo derivatives in the androstane and estrane series, 12-19, were synthesized by a fragmentation-cyclization reaction of 16-oximino-17-hydroxy-17-substituted derivatives 3-9, or by cyclization of the corresponding D-seco derivatives 20-26. The structures were confirmed by X-ray analysis of compounds 12 and 16. Preliminary assessment of inhibitory effects of D-homo derivatives from androstane series towards aromatase, 3 beta-hydroxysteroid dehydrogenase (3 beta-HSD), 17 alpha-hydroxylase/C17-20 lyase (P450c17) and 17 beta-HSD indicated much lower inhibitory potential compared to previously tested activity of another type of D-modified steroids, namely D-seco derivatives. Also, assessment of potential antiestrogenic activity of derivatives from estrane series showed absence of such an activity.
雄甾烷和雌甾烷系列中的D-高衍生物（12 - 19）是通过16-肟基-17-羟基-17-取代衍生物3 - 9的裂解环化反应，或通过相应的D-开环衍生物20 - 26的环化反应合成的。通过对化合物12和16的X射线分析确定了其结构。对雄甾烷系列D-高衍生物对芳香酶、3β-羟基类固醇脱氢酶（3β-HSD）、17α-羟化酶/C17-20裂解酶（P450c17）和17β-HSD的抑制作用的初步评估表明，与先前测试的另一种D-修饰类固醇即D-开环衍生物的活性相比，其抑制潜力要低得多。此外，对雌甾烷系列衍生物潜在抗雌激素活性的评估表明不存在这种活性。
