Discovery of imidazole vinyl pyrimidines as a novel class of kinase inhibitors which inhibit Tie-2 and are orally bioavailable

Tie-2 is a receptor tyrosine kinase which is involved in angiogenesis and thereby growth of human tumours. The discovery and SAR of a novel class of imidazole-vinyl-pyrimidine kinase inhibitors, which inhibit Tie-2 in vitro is reported. Their synthesis was carried out by condensation of imidazole aldehydes with methyl pyrimidines. These compounds are lead-like, with low molecular weight, good physical properties and oral bioavailability.

Graphical abstractThe discovery and SAR of a novel class of imidazole-alkene-pyrimidine kinase inhibitors, which inhibit Tie-2 in vitro and in cells is reported. These compounds are lead-like with low molecular weight and good physical properties, and are orally bioavailable.Figure optionsDownload full-size imageDownload as PowerPoint slide