Figadère B, Norman A W, Henry H L, Koeffler H P, Zhou J Y, Okamura W H
Department of Chemistry, University of California, Riverside 92521.
J Med Chem. 1991 Aug;34(8):2452-63. doi: 10.1021/jm00112a021.
Aromatic side-chain analogues (arocalciferols 6-9) of the steroid hormone 1 alpha,25-dihydroxyvitamin D3 (1) were synthesized and biologically evaluated. The analogues were prepared by coupling the vitamin D A-ring enyne 14 with the appropriate enol triflate of a modified CD steroid fragment of the type 22. The resulting dienyne 23 was then transformed in three steps to the vitamin D analogues 6-9. Biological evaluation of these analogues have provided information concerning side-chain topographical effects on in vivo and in vitro activity.
合成并生物学评价了甾体激素1α,25 - 二羟基维生素D3（1）的芳香族侧链类似物（芳基骨化醇6 - 9）。这些类似物是通过将维生素D A环烯炔14与22型修饰的CD甾体片段的适当烯醇三氟甲磺酸酯偶联制备的。然后将所得的二烯炔23通过三步转化为维生素D类似物6 - 9。对这些类似物的生物学评价提供了有关侧链拓扑结构对体内和体外活性影响的信息。
