26- and 27-Methyl groups of 2-substituted, 19-nor-1α,25-dihydroxylated vitamin D compounds are essential for calcium mobilization in vivo
作者： Pawel Grzywacz , Lori A. Plum , Margaret Clagett-Dame , Hector F. DeLuca
DOI: 10.1016/J.BIOORG.2013.01.001
关键词:
摘要: Twelve new analogs of 19-nor-1α,25-dihydroxyvitamin D36-17, were prepared by a multi-step procedure from known alcohols 18 and 19. We have examined the influence removing two methyl groups located at C-25, as well 25-hydroxy group, on biological in vitro vivo activity. Surprisingly, removal 26- 27-methyl either 2α-methyl or 2-methylene-19-nor-1α,25-dihydroxyvitamin D3 reduced vitamin D receptor binding, HL-60 differentiation, 25-hydroxylase transcription only slightly to moderately (compounds 6-13). However, these compounds devoid bone mobilization activity had markedly intestinal calcium transport. The 14-17 with 2β-methyl substitution little no expected previous work.
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