Synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK inhibitors with anti-angiogenic activity
作者： Pascal Dao , Rafika Jarray , Johanne Le Coq , Daniel Lietha , Ali Loukaci
DOI: 10.1016/J.BMCL.2013.06.038
关键词: Transferase 、 1,3,5-Triazine 、 Chemistry 、 Enzyme activator 、 Protein kinase domain 、 Inhibitory postsynaptic potential 、 Anti angiogenic 、 Kinase 、 Biochemistry 、 Focal adhesion 、 Organic chemistry 、 Clinical biochemistry 、 Molecular medicine 、 Molecular biology 、 Drug discovery 、 Pharmaceutical Science
摘要: We report herein the synthesis of novel diarylamino-1,3,5-triazine derivatives as FAK (focal adhesion kinase) inhibitors and evaluation their anti-angiogenic activity on HUVEC cells. Generally, effects these compounds endothelial cells could be correlated with kinase inhibitory activity. The most efficient displayed inhibition viability against in micromolar range, observed TAE-226, which was designed by Novartis Pharma AG. X-ray crystallographic analysis co-crystal structure for compound 34 revealed that mode interaction domain is highly similar to complex TAE-226.
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