Bioorganic and Medicinal Chemistry Letters p. 2145 - 2148 (1998)
Update date:2022-08-05
Topics:
Fujishima, Toshie
Liu, Zhaopeng
Miura, Daishiro
Chokki, Manabu
Ishizuka, Seiichi
Konno, Katsuhiro
Takayama, Hiroaki
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, 2α-methyl-20-epi-1α,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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