Highly potent cell differentiation-inducing analogues of 1α, 25-dihydroxyvitamin D 3: synthesis and biological activity of 2-methyl-1, 25-dihydroxyvitamin D 3 with side- …

T Fujishima, L Zhaopeng, K Konno, K Nakagawa…

文献索引：Fujishima, Toshie; Zhaopeng, Liu; Konno, Katsuhiro; Nakagawa, Kimie; Okano, Toshio; Yamaguchi, Kentaro; Takayama, Hiroaki Bioorganic and Medicinal Chemistry, 2001 , vol. 9, # 2 p. 525 - 535

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被引用次数: 33

摘要

Eight 2-methyl substituted analogues of 20-epi-22R-methyl-1α, 25-dihydroxyvitamin D3 (5) and 20-epi-24, 26, 27-trihomo-22-oxa-1α, 25-dihydroxyvitamin D3 (6: KH-1060) were convergently synthesized. Preparation of the CD-ring portions with modified side chains of 5 and 6, followed by palladium-catalyzed cross-coupling with the A-ring enyne synthons (20a– d),(3S, 4S, 5R)-,(3S, 4R, 5R)-,(3S, 4S, 5S)-and (3R, 4R, 5S)-3, 5-bis [(tert- ...