Difluoromethyl analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: Design, synthesis, and preliminary biological evaluation.
Difluoromethyl analogs of the natural hormone 1alpha,25-dihydroxyvitamin D3: Design, synthesis, and preliminary biological evaluation.
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天然激素 1α,25-二羟基维生素 D3 的二氟甲基类似物：设计、合成和初步生物学评估。
DOI：
10.1016/j.jsbmb.2006.12.024
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发表时间：
2007
期刊：
影响因子：
--
通讯作者：
Peleg,Sara
中科院分区：
文献类型：
--
作者：
Posner,GaryH;Suh,ByungChul;Petersen,KimberlyS;Dolan,Patrick;Agoston,ElinS;Kensler,ThomasW;Koh,JohnT;Peleg,Sara
合成了三种新的维生素D类似物3-5，其中含有-CHF 2基团作为-OH替代物。这些新的类似物中的两种（3和5）对鼠角质形成细胞具有强烈的抗增殖作用，并且在体内比天然激素骨化三醇的尿钙作用低约50倍。25-CHF 2类似物3的转录活性高于1-CHF 2类似物4。
Three new Vitamin D analogs 3–5 incorporating a –CHF2group 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-CHF2analog 3 is higher than that of the 1-CHF2analog 4.