Abstract Src kinase, a prototype member of the Src family of kinases (SFKs), is over- expressed in various human tumors, and has become a target for anticancer drug design. In this perspective, a series of eighteen 2-pyridone derivatives were synthesized and evaluated for their c-Src kinase inhibitory activity. Among them, eight compounds exhibited c- Src kinase inhibitory activity with IC 50 value of less than 25 μM. Compound 1-[2-( ...