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.
Rachid
Zakaria
Z
Cancer Drug Research Laboratory, Division of Medical Oncology, Department of Medicine, McGill University/Royal Victoria Hospital, 687 Pine Avenue west Rm M-719, Montreal, Québec, Canada H3A 1A1.
Brahimi
Fouad
F
Domarkas
Juozas
J
Jean-Claude
Bertrand Jacques
BJ
D018906:Antineoplastic Agents, Alkylating / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D066246:ErbB Receptors / Q000037:antagonists & inhibitors* / Q000737:chemistry; D005434:Flow Cytometry; D005453:Fluorescence; D006801:Humans; D020128:Inhibitory Concentration 50; D009363:Neoplasm Proteins / Q000037:antagonists & inhibitors; D009588:Nitrogen Mustard Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D018906:Antineoplastic Agents, Alkylating; D009363:Neoplasm Proteins; D009588:Nitrogen Mustard Compounds; D011799:Quinazolines; D066246:ErbB Receptors