Synthesis and biological activity of 2-methyl-20-epi analogues of 1 alpha,25-dihydroxyvitamin D3 |
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| Authors: | T Fujishima Z Liu D Miura M Chokki S Ishizuka K Konno H Takayama |
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| Affiliation: | Faculty of Pharmaceutical Sciences, Teikyo University, Kanagawa, Japan. |
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| 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. |
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