Synthesis of carbon-11-labeled tricyclic necroptosis inhibitors as new potential PET agents for imaging of tumor necrosis factor alpha (TNF-alpha).

Gao M; Lola CM; Wang M; Miller KD; Sledge GW; Hutchins GD; Zheng QH

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Synthesis of carbon-11-labeled tricyclic necroptosis inhibitors as new potential PET agents for imaging of tumor necrosis factor alpha (TNF-alpha).

机译：碳11标记的三环坏死性抑制剂的合成，作为用于肿瘤坏死因子α（TNF-alpha）成像的新型潜在PET试剂。

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Carbon-11-labeled tricyclic necroptosis inhibitors were first designed and synthesized as new potential PET agents for imaging of tumor necrosis factor alpha (TNF-alpha). The target tracers were prepared by O-[(11)C]methylation of their corresponding precursors using [(11)C]CH(3)OTf under basic conditions and isolated by a simplified SPE method in 50-60% radiochemical yields based on [(11)C]CO(2) and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 15-20 min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 111-185 GBq/micromol.

机译：碳11标记的三环坏死性抑制剂首先被设计并合成为用于肿瘤坏死因子α（TNF-alpha）成像的新的潜在PET剂。目标示踪剂是在碱性条件下，使用[（11）C] CH（3）OTf通过对其相应前体进行O-[（11）C]甲基化制备的，并通过简化的SPE方法以50-60％的放射化学收率进行分离[（11）C] CO（2）和衰变校正为轰炸（EOB）结束。 EOB的总合成时间为15-20分钟，放射化学纯度> 99％，合成结束时的比活（EOS）为111-185 GBq / micromol。

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《Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine》 |2010年第10期|共9页
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Gao M; Lola CM; Wang M; Miller KD; Sledge GW; Hutchins GD; Zheng QH;
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正文语种 eng
中图分类放射医学;
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1. Synthesis of carbon-11-labeled tricyclic necroptosis inhibitors as new potential PET agents for imaging of tumor necrosis factor alpha (TNF-alpha). [J] . Gao M, Lola CM, Wang M, Applied radiation and isotopes: including data, instrumentation and methods for use in agriculture, industry and medicine . 2010,第10期

机译：碳11标记的三环坏死性抑制剂的合成，作为用于肿瘤坏死因子α（TNF-alpha）成像的新型潜在PET试剂。
2. Design and synthesis of carbon-11-labeled dual aromatase-steroid sulfatase inhibitors as new potential PET agents for imaging of aromatase and steroid sulfatase expression in breast cancer. [J] . Wang M, Mickens J, Gao M Steroids: An International Journal . 2009,第12期

机译：碳11标记的双芳香酶-甾族硫酸酯酶抑制剂的设计与合成，作为乳腺癌中芳香酶和甾族硫酸酯酶表达成像的新型潜在PET试剂。
3. Substituted isoquinolines and quinazolines as potential antiinflammatory agents. Synthesis and biological evaluation of inhibitors of tumor necrosis factor alpha. [J] . Chao Q, Deng L, Shih H, Journal of Medicinal Chemistry . 1999,第19期

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4. DETECTION OF TUMOR NECROSIS FACTOR ALPHA (TNF-ALPHA) IN DOGS WITH LYMPHOMA [C] . Jennifer Hofer, Mark Papich, Teresa DeFrancesco, Annual Conference of the Veterinary Cancer Society . 2009

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5. The role of tumor necrosis factor alpha (TNF-alpha) in the eyes and brain of HSV-1 infected euthymic BALB/c mice. [D] . Fields, Mark A. 2007

机译：肿瘤坏死因子α（TNF-alpha）在HSV-1感染的正常BALB / c小鼠的眼睛和大脑中的作用。
6. Jun N-terminal kinase/stress-activated protein kinase (JNK/SAPK) is required for lipopolysaccharide stimulation of tumor necrosis factor alpha (TNF-alpha) translation: glucocorticoids inhibit TNF-alpha translation by blocking JNK/SAPK. [O] . J L Swantek, M H Cobb, T D Geppert 1997

机译：Jun N端激酶/应激激活蛋白激酶（JNK / SAPK）是脂多糖刺激肿瘤坏死因子α（TNF-alpha）翻译所必需的：糖皮质激素通过阻断JNK / SAPK抑制TNF-alpha翻译。
7. Jun N-terminal kinase/stress-activated protein kinase (JNK/SAPK) is required for lipopolysaccharide stimulation of tumor necrosis factor alpha (TNF-alpha) translation: glucocorticoids inhibit TNF-alpha translation by blocking JNK/SAPK. [O] . Swantek, J L, Cobb, M H, Geppert, T D 1997

机译：Jun N端激酶/应激激活蛋白激酶（JNK / SAPK）是脂多糖刺激肿瘤坏死因子α（TNF-alpha）翻译所必需的：糖皮质激素通过阻断JNK / SAPK抑制TNF-alpha翻译。
8. Hantaan Virus Nucleocapsid Protein Binds to Importin alpha Proteins and Inhibits Tumor Necrosis Factor Alpha-Induced Activation of Nuclear Factor Kappa B [R] . Taylor, S. L., Frias-Staheli, N., Garcia-Sastre, A., 2008

机译：汉坦病毒核衣壳蛋白与进口蛋白α蛋白结合并抑制肿瘤坏死因子α诱导的核因子κB活化

Synthesis of carbon-11-labeled tricyclic necroptosis inhibitors as new potential PET agents for imaging of tumor necrosis factor alpha (TNF-alpha).

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