Synthesis of half-mustard combi-molecules with fluorescence properties: correlation with EGFR status

The synthesis of 6-(2-chloroethylamino)-4-anilinoquinazolines (ZR2002 and ZR2003) designed to block EGFR tyrosine kinase and to damage genomic DNA is described. These compounds present fluorescence properties that permitted the quantitation of their subcellular uptake by flow cytometry. Fluorescence intensities increased with increasing levels of EGFR in a panel of isogenic and established cell lines.