Synthesis of novel 1alpha,25-dihydroxy-19-norvitamin D_3 with an amide conjucate

摘要

The Diene system of 1alpha,25-dihydroxy-19-norvitamin D_3 was replaced by a stable amide bond.A3-hydroxypropoxy group,which was effective on enhancing binding affinity f 1alpha,25-dihydroyvitamin D_3 for vitamin Dreceptor (VDR),was introduced to the 2-position of the amide type analogue of 1alpha,25-dihydroxy-19-norvitamin D_3.the amide analogue was found to be not suitable for binding to the ligand binding domain of the bovine thymus VDR,and additional modificatin at the C2-position did not improve the affinity.Potency in induction of HL-60 cell differentiatin was evaluated for the novel amide analogues (3a-c).