The synthesis and SAR of new 4-(N-alkyl-N-phenyl)amino-6,7-dimethoxyquinazolines and 4-(N-alkyl-N-phenyl)amino-pyrazolo[3,4-d]pyrimidines, inhibitors of CSF-1R tyrosine kinase activity

Article abstract of DOI:10.1016/S0960-894X(97)00035-8

We have identified moderately potent and selective inhibitors of CSF-1R tyrosine kinase activity. 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.