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ID: ALA1143991

Journal: Bioorg Med Chem

Title: The 2alpha-(3-hydroxypropyl) group as an active motif in vitamin D3 analogues as agonists of the mutant vitamin D receptor (Arg274Leu).

Authors: Honzawa S, Yamamoto Y, Yamashita A, Sugiura T, Kurihara M, Arai MA, Kato S, Kittaka A.

Abstract: We designed and synthesized 1alpha- and 1beta-hydroxymethyl-2alpha-(3-hydroxypropyl)-25-hydroxyvitamin D(3) (2a,b) and related analogues 2alpha-(3-hydroxypropyl)-25-hydroxyvitamin D(3) (3), Posner's analogues of 1alpha- and 1beta-hydroxymethyl-25-hydroxyvitamin D(3) (4a,b), as well as 2alpha-(3-hydroxypropyl)-1alpha,25-dihydroxyvitamin D(3) (5), to confirm the effect of the 1alpha-hydroxy group and/or 2alpha-(3-hydroxypropyl) group of vitamin D(3) analogues with the modified A-ring moiety on the mutant vitamin D receptor, VDR(Arg274Leu). The 2alpha-(3-hydroxypropyl) group showed better effect on enhancement of the transcriptional activity through the mutant VDR than the 1alpha- and 1beta-hydroxymethyl groups.

CiteXplore: 18248997

DOI: 10.1016/j.bmc.2007.12.039