Mono-and Dihydroxylated Metabolites of Thalidomide:Synthesis and TNF-alpha Production-Inhibitory Activity

Takanori NAKAMURA; Tomomi NOGUCHI; Hisayoshi KOBAYASHI

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Mono-and Dihydroxylated Metabolites of Thalidomide:Synthesis and TNF-alpha Production-Inhibitory Activity

机译：沙利度胺的单和二羟基化代谢产物：合成和TNF-α生产抑制活性。

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摘要

Mono-and dihydroxylated metabolites of thalidomide were efficiently prepared and characterized,and their inhibitory activity on tumor necrosis factor (TNF)-alpha production in the human monocytic leukemia cell line THP-1 was evaluated.5,N-Dihydroxythalidomide was a much more potent TNF-a production inhibitor than thalidomide.

机译：有效地制备和表征了沙利度胺的单羟基和二羟基化代谢产物，并评估了它们对人单核细胞白血病细胞系THP-1中肿瘤坏死因子（TNF）-α产生的抑制活性。5，N-二羟基沙利度胺具有更强的效力TNF-α产生抑制剂比沙利度胺。

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来源
《Journal of Medicinal Chemistry》 |2007年第26期|共6页
作者
Takanori NAKAMURA; Tomomi NOGUCHI; Hisayoshi KOBAYASHI;
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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
thalidomide; hydroxythalidomide; metabolite; tumor necrosis factor (TNF)-alpha modulator;

机译：沙利度胺;羟基沙利度胺;代谢物;肿瘤坏死因子（TNF）-α调节剂;

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专利

1. Mono-and Dihydroxylated Metabolites of Thalidomide:Synthesis and TNF-alpha Production-Inhibitory Activity [J] . Takanori NAKAMURA, Tomomi NOGUCHI, Hisayoshi KOBAYASHI Journal of Medicinal Chemistry . 2007,第26期

机译：沙利度胺的单和二羟基化代谢产物：合成和TNF-α生产抑制活性。
2. Mono- and dihydroxylated metabolites of thalidomide: Synthesis and TNF-alpha production-inhibitory activity [J] . Nakamura T, Noguchi T, Kobayashi H, Chemical and Pharmaceutical Bulletin . 2006,第12期

机译：沙利度胺的单羟基和二羟基化代谢产物：合成和TNF-α生产抑制活性
3. Hydrolyzed metabolites of thalidomide: synthesis and TNF-alpha production-inhibitory activity. [J] . Nakamura T, Noguchi T, Miyachi H, Chemical and Pharmaceutical Bulletin . 2007,第4期

机译：沙利度胺的水解产物：合成和TNF-α生产抑制活性。
4. Metabolites of Thalidomide Using the Humanized CYP3A Transchromosomic Mouse Liver Microsome, Detected by LC-MS/MS system [C] . Shin-ichiro Nitta, Yasuko Tsukazaki, Naoto Senda, American Society for Mass Spectrometry Conference on Mass Spectrometry and Allied Topics . 2011

机译：使用LC-MS / MS系统检测的人源化CYP3A转斜圆锥组种小鼠肝微小肝微小羟基核素小鼠肝微粒的代谢物
5. Synthesis, reactivity, and bioactivation screening of potential carcinogenic metabolites of triphenylethylene antiestrogens. [D] . Fan, Peter Wei-Jen. 2001

机译：三苯乙烯抗雌激素的潜在致癌代谢产物的合成，反应性和生物活化筛选。
6. In vivo Formation of Dihydroxylated and Glutathione Conjugate Metabolites derived from Thalidomide and 5-Hydroxythalidomide in Humanized TK-NOG mice [O] . Hiroshi Yamazaki, Hiroshi Suemizu, Makiko Shimizu, -1

机译：在二羟基化和谷胱甘肽共轭代谢物的体内形成在人源化TK-NOG小鼠免于沙利度胺和5- Hydroxythalidomide衍生
7. Hydrolyzed Metabolites of Thalidomide: Synthesis and TNF-.ALPHA. Production-Inhibitory Activity [O] . Takanori Nakamura, Tomomi Noguchi, Hiroyuki Miyachi, 2007

机译：水解的沙利度胺：合成和TNF-alpha的水解代谢物。生产抑制活性
8. Synthesis and Antimuscarinic Activity of 2-(N-(Ethyl)-(N-Beta-Hydroxyethyl))Aminoethyl 2,2-Diphenylpropionate, a Metabolite of Aprophen [R] . Brown, N. D., Leader, H., Phillips, L. R., 1993

机译：2-（N-（乙基） - （N-β-羟乙基））氨基乙基2,2-二苯基丙酸酯的合成及抗毒活性，二苯丙酸代谢物

Mono-and Dihydroxylated Metabolites of Thalidomide:Synthesis and TNF-alpha Production-Inhibitory Activity

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