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2-(Quinazolin-4-ylamino)-[1,4]benzoquinones as covalent-binding, irreversible inhibitors of the kinase domain of vascular endothelial growth factor receptor-2.2-（喹唑啉-4-基氨基）-[1,4]苯醌作为血管内皮生长因子受体-2激酶结构域的共价结合、不可逆抑制剂。
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Potent, selective and low-calcemic inhibitors of CYP24 hydroxylase: 24-sulfoximine analogues of the hormone 1alpha,25-dihydroxyvitamin D(3).CYP24羟化酶的强效、选择性和低钙血症抑制剂：激素1α,25-二羟基维生素D(3)的24-亚磺酰亚胺类似物。
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Low-calcemic, efficacious, 1alpha,25-dihydroxyvitamin D3 analog QW-1624F2-2: calcemic dose-response determination, preclinical genotoxicity testing, and revision of A-ring stereochemistry.
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Efficient synthesis of the A-ring phosphine oxide building block useful for 1 alpha,25-dihydroxy vitamin D(3) and analogues.用于1α,25 - 二羟基维生素D(3)及其类似物的A环氧化膦结构单元的高效合成。
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Antiproliferative Hybrid Analogs of the Hormone 1alpha,25-Dihydroxyvitamin D(3): Design, Synthesis, and Preliminary Biological Evaluation.激素1α,25-二羟基维生素D(3)的抗增殖杂合类似物：设计、合成及初步生物学评价
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Noncalcemic, antiproliferative, transcriptionally active, 24-fluorinated hybrid analogues of the hormone 1alpha, 25-dihydroxyvitamin D3. Synthesis and preliminary biological evaluation.激素1α,25-二羟基维生素D3的非钙调节、抗增殖、具有转录活性的24-氟代杂合类似物。合成及初步生物学评价。
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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.

DOI:10.1016/j.jsbmb.2006.12.024
PMID:17218093
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2712873/
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。