2-Aminoquinazoline inhibitors of cyclin-dependent kinases.
The inhibition of cyclin-dependent kinase 4 (Cdk4) causes cell cycle arrest and restores a checkpoint that is absent in the majority of tumor cells. Compounds that inhibit Cdk4 selectively are targeted for treating cancer. Appropriate substitution of 2-aminoquinazolines is demonstrated to produce high levels of selectivity for Cdk4 versus closely related serine-threonine kinases.
NAEJA Pharmaceutical Inc., #2, 4290-91A Street, Edmonton, Alberta, Canada T65VE.
Yadagiri
Y
Bathini
Inderjit
I
Singh
Patricia J
PJ
Harvey
Paul R
PR
Keller
Rajeshwar
R
Singh
Ronald G
RG
Micetich
David W
DW
Fry
Ellen M
EM
Dobrusin
Peter L
PL
Toogood
D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D051358:Cyclin-Dependent Kinase 4; D018844:Cyclin-Dependent Kinases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D011518:Proto-Oncogene Proteins / Q000037:antagonists & inhibitors*; D011799:Quinazolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011518:Proto-Oncogene Proteins; D011799:Quinazolines; C495900:CDK4 protein, human; D051358:Cyclin-Dependent Kinase 4; D018844:Cyclin-Dependent Kinases