天然激素1α,25 - 二羟基维生素D3的二氟甲基类似物：设计、合成及初步生物学评价
Difluoromethyl analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: Design, synthesis, and preliminary biological evaluation.
作者信息
Posner Gary H, Suh Byung Chul, Petersen Kimberly S, Dolan Patrick, Agoston Elin S, Kensler Thomas W, Koh John T, Peleg Sara
机构信息
Department of Chemistry, The Johns Hopkins University, Baltimore, MD 21218, USA.
出版信息
J Steroid Biochem Mol Biol. 2007 Mar;103(3-5):213-21. doi: 10.1016/j.jsbmb.2006.12.024. Epub 2007 Jan 10.
Abstract
Three new Vitamin D analogs 3-5 incorporating a -CHF(2) group as an -OH surrogate have been prepared. Two of these new analogs (3 and 5) are strongly antiproliferative toward murine keratinocytes and are approximately 50 times less calciuric in vivo than the natural hormone calcitriol. The transcriptional activity of the 25-CHF(2) analog 3 is higher than that of the 1-CHF(2) analog 4.
摘要
已经制备了三种新的维生素D类似物3-5，它们引入了-CHF(2)基团作为-OH替代物。其中两种新类似物（3和5）对小鼠角质形成细胞具有强烈的抗增殖作用，并且在体内的钙尿活性比天然激素骨化三醇低约50倍。25-CHF(2)类似物3的转录活性高于1-CHF(2)类似物4。
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