کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1374041 | 981912 | 2012 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Utilization of [11C]phosgene for radiosynthesis of N-(2-{3-[3,5-bis(trifluoromethyl)]phenyl[11C]ureido}ethyl)glycyrrhetinamide, an inhibitory agent for proteasome and kinase in tumors Utilization of [11C]phosgene for radiosynthesis of N-(2-{3-[3,5-bis(trifluoromethyl)]phenyl[11C]ureido}ethyl)glycyrrhetinamide, an inhibitory agent for proteasome and kinase in tumors](/preview/png/1374041.png)
N-(2-{3-[3,5-Bis(trifluoromethyl)]phenylureido}ethyl)glycyrrhetinamide (2), an ureido-substituted derivative of glycyrrhetinic acid (1), has been reported to display potent inhibitory activity for proteasome and kinase, which are overexpressed in tumors. In this study, we labeled this unsymmetrical urea 2 using [11C]phosgene ([11C]COCl2) as a labeling agent with the expectation that [11C]2 could become a positron emission tomography ligand for the imaging of proteasome and kinase in tumors. The strategy for the radiosynthesis of [11C]2 was to react hydrochloride of 3,5-bis(trifluoromethyl)aniline (4·HCl) with [11C]COCl2 to possibly give isocyanate [11C]6, followed by the reaction of [11C]6 with N-(2-aminoethyl)glycyrrhetinamide (3).
Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 11, 1 June 2012, Pages 3594–3597