Discovery and evaluation of 3-phenyl-1H-5-pyrazolylamine-based derivatives as potent, selective and efficacious inhibitors of FMS-like tyrosine kinase-3 (FLT3)

► We identified 3-phenyl-1H-5-pyrazolylamine-based derivatives as FLT3 inhibitors. ► These derivatives contain benzamide series and pyrimidine series. ► Pyrimidine 12a is highly selective for FLT3 over the closely related kinases. ► Pyrimidine 12a showed highly antitumor efficacy in the human AML xenograft models.