Title of article :
The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)aminopyrazolo[3,4-d]pyrimidines, inhibitors of CSF-1R tyrosine kinase activity
Author/Authors :
Michael R. Myers، نويسنده , , Natalie N. Setzer، نويسنده , , Alfred. P. Spada، نويسنده , , Paul E. Persons، نويسنده , , Cuong Q. Ly، نويسنده , , Martin P. Maguire، نويسنده , , Allison L. Zulli، نويسنده , , Daniel L. Cheney، نويسنده , , Asher Zilberstein، نويسنده , , Susan E. Johnson، نويسنده , , Carol F. Franks، نويسنده , , Karen J. Mitchell، نويسنده ,
Abstract :
We have identified moderately potent and selective inhibitors of CSF-1R tyrosine kinase activity.1 A preliminary SAR study resulted in the identification of compounds 11 and 20 as the most potent analogues in the series (IC50 = 0.18 μM). The 3-D-conformation of the 4-(N-alkyl-N-phenyl)-aminoquinazolines has been proposed to be important to the overall selectivity and activity.
