放射性碘化嘧啶-2,4,6-三酮的合成作为基质金属蛋白酶非侵入性成像的潜在试剂
Syntheses of Radioiodinated Pyrimidine-2,4,6-Triones as Potential Agents for Non-Invasive Imaging of Matrix Metalloproteinases.
作者信息
Breyholz Hans-Jörg, Kopka Klaus, Schäfers Michael, Wagner Stefan
机构信息
Department of Nuclear Medicine, University Hospital Münster, Albert-Schweitzer-Campus 1, Building A1, D-48149 Münster, Germany.
Division of Radiopharmaceutical Chemistry, German Cancer Research Center (DKFZ), Im Neuenheimer Feld 280, D-69120 Heidelberg, Germany.
出版信息
Pharmaceuticals (Basel). 2017 May 30;10(2):49. doi: 10.3390/ph10020049.
Dysregulated expression or activation of matrix metalloproteinases (MMPs) is observed in many kinds of live-threatening diseases. Therefore, MMP imaging for example with radiolabelled MMP inhibitors (MMPIs) potentially represents a valuable tool for clinical diagnostics using non-invasive single photon emission computed tomography (SPECT) or positron emission tomography (PET) imaging. This work includes the organic chemical syntheses and in vitro evaluation of five iodinated barbiturate based MMPIs and the selection of derivative for radiosyntheses of isotopologues [I] potentially useful for MMP SPECT imaging and [I] for MMP PET imaging.
在许多危及生命的疾病中都观察到基质金属蛋白酶（MMPs）的表达失调或激活。因此，例如使用放射性标记的MMP抑制剂（MMPIs）进行MMP成像，可能代表了一种使用非侵入性单光子发射计算机断层扫描（SPECT）或正电子发射断层扫描（PET）成像进行临床诊断的有价值工具。这项工作包括五种基于碘化巴比妥酸盐的MMPIs的有机化学合成和体外评估，以及选择用于同位素类似物[I]的放射性合成的衍生物，[I]可能用于MMP SPECT成像，[I]用于MMP PET成像。
Zotero 插件