Schepens Wim, Van Haver Dirk Van, Vandewalle Maurits, De Clercq Pierre J, Bouillon Roger, Verstuyf Annemieke
Department of Organic Chemistry, Ghent University, Krijgslaan 281 S4, B-9000 Gent, Belgium.
Bioorg Med Chem Lett. 2004 Aug 2;14(15):3889-92. doi: 10.1016/j.bmcl.2004.05.058.
The synthesis and biological activity of novel CD-ring modified analogues of 22-oxa-1alpha,25-dihydroxyvitamin D(3), lacking the D-ring and featuring a connection between C-18 and C-21 (spiro[5.5]undecane CF-ring analogues), is described. The central ring system is conveniently synthesised from an achiral intermediate. The analogues have marginal binding affinity for the nVDR and possess low to moderate genomic activity.
描述了新型22-氧杂-1α,25-二羟基维生素D(3)的CD环修饰类似物的合成及生物活性，这些类似物缺少D环，且在C-18和C-21之间有连接（螺[5.5]十一烷CF环类似物）。中心环系统可方便地由非手性中间体合成。这些类似物对nVDR的结合亲和力较低，基因组活性为低到中等。
