Justice J B
J Med Chem. 1978 May;21(5):465-8. doi: 10.1021/jm00203a011.
A Fujita--Ban structure--activity analysis has been performed on 44 steroids with a common pregn-4-ene-3,20-dione structure. The measured biological activity was glycogen deposition in the liver, expressed relative to the activity of cortisol. Substituents are at positions 2, 6, 9alpha, 11beta, 16alpha, 17, and 21. Substituents of positions 2, 6, and 17 accounted for 60% of the total variance. The substituents with significance at the p less than 0.01 level were 6alpha-hydrogen, 6alpha-methyl, 2alpha-hydrogen, 9alpha-fluorine, and 9alpha-hydrogen.
已对44种具有共同孕-4-烯-3,20-二酮结构的甾体进行了藤田-班结构-活性分析。所测生物活性为肝脏中的糖原沉积,相对于皮质醇的活性表示。取代基位于2、6、9α、11β、16α、17和21位。2、6和17位的取代基占总方差的60%。在p小于0.01水平具有显著性的取代基为6α-氢、6α-甲基、2α-氢、9α-氟和9α-氢。