The synthesis of 1-[4-(m-tolyl)amino-6-quinazolinyl]-3-[14C]-methyl triazene (SMA41) is described. This triazene was designed to be hydrolyzed under physiological conditions to N4-m-tolyl-quinazoline-4,6-diamine (SMA52), a moderate inhibitor of the epidermal growth factor receptor (EGFR) and the DNA alkylating species [14C]-methyldiazonium. A radiolabeled probe was needed to test the hypothesis that in situ hydrolysis of SMA41 may induce alkylation of the ATP binding site of EGFR. 14C-SMA41 was obtained with a radiochemical yield of 21% and a specific activity of 54.6 mCi/mmol, as determined by HPLC quantitation and scintillation counting. Radio-TLC analyses showed 98% radiochemical purity. Copyright © 2003 John Wiley & Sons, Ltd.
本文介绍了 1-[4-(间
甲苯基)
氨基-6-
喹唑啉基]-3-[14C]-甲基三嗪(SMA41)的合成。这种三嗪被设计成在生理条件下
水解成 N4-间
甲苯基
喹唑啉-4,6-二胺(SMA52),它是
表皮生长因子受体(
EGFR)和 DNA 烷基化物种 [14C]-methyldiazonium 的中度
抑制剂。我们需要一种放射性标记探针来验证 SMA41 原位
水解可能诱导
表皮生长因子受体
ATP 结合位点烷基化的假设。经 HPLC 定量和闪烁计数测定,14C-SMA41 的放射
化学收率为 21%,比活度为 54.6 mCi/mmol。放射性-
液相色谱分析显示放射性纯度为 98%。Copyright © 2003 John Wiley & Sons, Ltd. All Rights Reserved.