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ID: ALA1130923

Journal: Bioorg Med Chem Lett

Title: Synthesis and biological activity of 2-methyl-20-epi analogues of 1 alpha,25-dihydroxyvitamin D3.

Authors: Fujishima T, Liu Z, Miura D, Chokki M, Ishizuka S, Konno K, Takayama H.

Abstract: Synthesis and biological evaluation of all eight possible A-ring diastereomers of 2-methyl-20-epi-1,25-dihydroxyvitamin D3 are described. Among the analogues synthesized. 2 alpha-methyl-20-epi-1 alpha,25-dihydroxyvitamin D3 exhibited exceptionally high potency. The double modification of 2-methyl substitution and 20-epimerization yielded analogues with unique activity profiles.

CiteXplore: 9873502

DOI: 10.1016/s0960-894x(98)00363-1