Novel 4-anilinoquinazolines with C-6 carbon-linked side chains: Synthesis and structure–activity relationship of a series of potent, orally active, EGF receptor tyrosine kinase inhibitors

The structure–activity relationship of a novel subseries of 4-anilinoquinazoline EGFR inhibitors substituted at the C-6 position with carbon-linked side chains has been investigated. This exploration has led to the discovery of novel aminomethyl carboxamides with good biological, pharmacokinetic and physical properties.

Graphical abstractThe discovery and SAR of a novel subseries of 4-anilinoquinazoline EGFR inhibitors substituted at the C-6 position with carbon-linked side chains are described.Figure optionsDownload full-size imageDownload as PowerPoint slide