763123-75-7Relevant academic research and scientific papers
New heterocyclic analogues of 4-(2-chloro-5-methoxyanilino)quinazolines as potent and selective c-Src kinase inhibitors
Barlaam, Bernard,Fennell, Mike,Germain, Herve,Green, Tim,Hennequin, Laurent,Morgentin, Remy,Olivier, Annie,Ple, Patrick,Vautier, Michel,Costello, Gerard
, p. 5446 - 5449 (2007/10/03)
A series of 5,7-disubstituted quinazolines, bearing 4-heteroaryl substituents such as 2-pyridinylamine or 2-pyrazinylamine, has been synthetised and evaluated as c-Src kinase inhibitors. Highly potent inhibition, high selectivity and physical properties suitable for oral dosing were achieved within this series: 23d and 42 were identified as sub-0.1 μM inhibitors in a c-Src-driven cell proliferation assay and displayed adequate rat pharmacokinetics after oral administration.
