Synthesis of 1-[4-(m-tolyl)amino-6-quinazolinyl]-3-[14C]-methyl triazene: a radiolabeled probe for the combi-targeting concept
作者： Stephanie L. Matheson , Shadreck Mzengeza , Bertrand J. Jean-Claude
DOI: 10.1002/JLCR.713
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摘要: The synthesis of 1-[4-(m-tolyl)amino-6-quinazolinyl]-3-[14C]-methyl triazene (SMA41) is described. This was designed to be hydrolyzed under physiological conditions N4-m-tolyl-quinazoline-4,6-diamine (SMA52), a moderate inhibitor the epidermal growth factor receptor (EGFR) and DNA alkylating species [14C]-methyldiazonium. A radiolabeled probe needed test hypothesis that in situ hydrolysis SMA41 may induce alkylation ATP binding site EGFR. 14C-SMA41 obtained with radiochemical yield 21% specific activity 54.6 mCi/mmol, as determined by HPLC quantitation scintillation counting. Radio-TLC analyses showed 98% purity. Copyright © 2003 John Wiley & Sons, Ltd.
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