Synthesis of pyrimidinopyridine-triazene conjugates targeted to abl tyrosine kinase.
The synthesis and abl tyrosine kinase inhibitory activities of alkyltriazenes conjugated to phenylaminopyrimidines are described. Significant abl inhibitory activities were observed only when a benzamido spacer was inserted between the 1,2,3-triazene chain and the 2-phenyaminopyridopyrimidine moiety.
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.
Katsoulas
Athanasia
A
Brahimi
Fouad
F
Jean-Claude
Bertrand Jacques
BJ
D016503:Drug Delivery Systems / Q000379:methods*; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000138:chemical synthesis; D016044:Fusion Proteins, bcr-abl; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011725:Pyridines / Q000008:administration & dosage / Q000138:chemical synthesis*; D011744:Pyrimidinones / Q000008:administration & dosage / Q000138:chemical synthesis*; D014226:Triazenes / Q000008:administration & dosage / Q000138:chemical synthesis*
D004791:Enzyme Inhibitors; D011725:Pyridines; D011744:Pyrimidinones; D014226:Triazenes; D011505:Protein-Tyrosine Kinases; D016044:Fusion Proteins, bcr-abl