Highly antiproliferative, low-calcemic, side-chain amide and hydroxamate analogs of the hormone 1alpha,25-dihydroxyvitamin D3.
Highly antiproliferative, low-calcemic, side-chain amide and hydroxamate analogs of the hormone 1alpha,25-dihydroxyvitamin D3.
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激素 1α,25-二羟基维生素 D3 的高度抗增殖、低钙血症、侧链酰胺和异羟肟酸酯类似物。
DOI：
10.1016/j.bmc.2006.05.050
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发表时间：
2006
影响因子：
3.5
通讯作者：
Posner,GaryH
中科院分区：
文献类型：
--
作者：
Sinishtaj,Sandra;Jeon,HeungBae;Dolan,Patrick;Kensler,ThomasW;Posner,GaryH
合成了激素骨化三醇(1)的四个新的侧链酰胺(2和3)和异羟甲酸酯(4和5)类似物。尽管缺少天然骨化三醇(1)所特有的25-OH基团，类似物2-4在体外与骨化三醇(1)一样具有抗增殖作用，但体内的钙尿量比骨化三醇(1)少20-40倍。
Four new side-chain amide (2 and 3) and hydroxamate (4 and 5) analogs of the hormone calcitriol (1) have been prepared. Even though lacking the 25-OH group characteristic of natural calcitriol (1), analogs 2–4 are as antiproliferative in vitro as calcitriol (1) but are 20–40 times less calciuric in vivo than calcitriol (1).