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

作者信息

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

机构信息

Faculty of Pharmaceutical Sciences, Teikyo University, Kanagawa, Japan.

出版信息

Bioorg Med Chem Lett. 1998 Aug 18;8(16):2145-8. doi: 10.1016/s0960-894x(98)00363-1.

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.