SYNTHESIS OF 26,27-DIALKYL ANALOGS OF 1-ALPHA,25-DIHYDROXYVITAMIN D3

被引:0
|
作者
EGUCHI, T [1 ]
SAI, H [1 ]
TAKATSUTO, S [1 ]
HARA, N [1 ]
IKEKAWA, N [1 ]
机构
[1] TOKYO INST TECHNOL, DEPT CHEM, TOKYO 152, JAPAN
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中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
1.alpha.,25-Dihydroxy-26,27-dimethylvitamin D3 (5), 1.alpha.,25-dihydroxy-26,27-diethylvitamin D3 (6), 25-hydroxy-26,27-dimethylvitamin D3 (7), and 1.alpha.-hydroxy-26,27-dimethylvitamin D3 (8), as dialkyl analogues of 1.alpha.,25-dihydroxyvitamin D3 (1), were synthesized starting from 3.beta.-hydroxycholenic acid (9). When tested for ability to increase serum calcium concentration in rats, 5 was slightly less active than 1, whereas 6 was much less active. Compound 8 was less active than 1.alpha.-hydroxyvitamin D3. In test for ability to induce cell differentiation of HL-60, 5 was 2.5 times and 6 was 12.5 times more active than 1.
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页码:2303 / 2311
页数:9
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