Novel A-ring analogs of the hormone 1α,25-dihydroxyvitamin D3:: synthesis and preliminary biological evaluation

被引:13
作者
Posner, GH
Lee, SHT
Kim, HJ
Peleg, S
Dolan, P
Kensler, TW
机构
[1] Johns Hopkins Univ, Dept Chem, Baltimore, MD 21218 USA
[2] Univ Texas, MD Anderson Canc Ctr, Dept Med Specialties, Houston, TX 77030 USA
[3] Johns Hopkins Univ, Bloomberg Sch Publ Hlth, Div Environm Hlth Sci, Baltimore, MD 21205 USA
关键词
vitamin D analogs; SAR; growth inhibition;
D O I
10.1016/j.bmc.2005.02.005
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 [生物化学与分子生物学]; 081704 [应用化学];
摘要
Prepared from a commercial prostaglandin building block, novel vitamin D-3 analogs with a contracted five-membered A-ring were designed and synthesized to mimic the A-ring diol structure of the natural hormone lot,1 alpha,25-dihydroxyvitamin D-3- Prepared from commercial 1,4-cyclohexanedione, a structurally simplified analog was designed and synthesized in which a suitably oriented primary allylic hydroxyl group at the C-2 position might be a surrogate for the biologically important lot-OH in the natural hormone. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:2959 / 2966
页数:8
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