Discovery and preliminary structure–activity relationship studies of novel benzotriazine based compounds as Src inhibitors

We report the discovery and preliminary SAR studies of a series of structurally novel benzotriazine core based small molecules as inhibitors of Src kinase. To the best of our knowledge, benzotriazine template based compounds have not been reported as kinase inhibitors. The 3-(2-(1-pyrrolidinyl)ethoxy)phenyl analogue (43) was identified as one of the most potent inhibitors of Src kinase.

Graphical abstractWe report the SAR studies of a series of structurally novel benzotriazine analogs as inhibitors of Src. The 3-(2-(1-pyrrolidinyl)-ethoxy)phenyl analog (43) was identified as one of the most potent inhibitors.Figure optionsDownload full-size imageDownload as PowerPoint slide