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

DOI: 10.1016/S0960-894X(98)00363-1

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 2145 - 2148 (1998)

Update date:2022-08-05

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Authors:

Fujishima, Toshie

Liu, Zhaopeng

Miura, Daishiro

Chokki, Manabu

Ishizuka, Seiichi

Konno, Katsuhiro

Takayama, Hiroaki

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Article abstract of 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, 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.

Full text of DOI:10.1016/S0960-894X(98)00363-1

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