a b s t r a c t
A series of N0-(2-oxoindolin-3-ylidene)hydrazide derivatives were identified as moderately potent inhibitors
against c-Met kinase by pharmacophore-based virtual screening and chemical synthesis methods.
The structure–activity relationship (SAR) at various positions of the scaffold was investigated and its
binding mode with c-Met kinase was analyzed by molecular modeling studies. In this study, two potent
compounds D2 and D25, with IC50 value at 1.3 lM and 2.2 lM against c-Met kinase respectively, were
identified. Finally, based on the clues extracted from this study, future development for the optimization
of this scaffold was discussed.