AI Article Synopsis
- - A new compound, N-(2-{3-[3,5-Bis(trifluoromethyl)]phenylureido}ethyl)glycyrrhetinamide, is derived from glycyrrhetinic acid and shows strong inhibiting effects on proteins that are overly produced in tumors, specifically proteasomes and kinases.
- - The researchers aim to create a radiolabeled version of this compound, referred to as [(11)C]2, for use in positron emission tomography (PET) to visualize these proteins in tumors.
- - The method for synthesizing [(11)C]2 involves a series of chemical reactions, starting with the interaction of a specific hydrochloride compound with a carbon-11 labeled
Article Abstract
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 [(11)C]phosgene ([(11)C]COCl(2)) as a labeling agent with the expectation that [(11)C]2 could become a positron emission tomography ligand for the imaging of proteasome and kinase in tumors. The strategy for the radiosynthesis of [(11)C]2 was to react hydrochloride of 3,5-bis(trifluoromethyl)aniline (4·HCl) with [(11)C]COCl(2) to possibly give isocyanate [(11)C]6, followed by the reaction of [(11)C]6 with N-(2-aminoethyl)glycyrrhetinamide (3).
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| http://dx.doi.org/10.1016/j.bmcl.2012.04.049 | DOI Listing |
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