1470249-17-2Relevant articles and documents
Substituted Quinazoline and Pyridopyrimidine Derivatives Useful as Anticancer Agents
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, (2019/08/22)
Compounds of the general formula: processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.
Design and evaluation of novel 8-oxo-pyridopyrimidine Jak1/2 inhibitors
Labadie, Sharada,Barrett, Kathy,Blair, Wade S.,Chang, Christine,Deshmukh, Gauri,Eigenbrot, Charles,Gibbons, Paul,Johnson, Adam,Kenny, Jane R.,Kohli, Pawan Bir,Liimatta, Marya,Lupardus, Patrick J.,Shia, Steven,Steffek, Micah,Ubhayakar, Savita,Abbema, Anne Van,Zak, Mark
, p. 5923 - 5930 (2013/10/22)
A highly ligand efficient, novel 8-oxo-pyridopyrimidine containing inhibitor of Jak1 and Jak2 isoforms with a pyridone moiety as the hinge-binding motif was discovered. Structure-based design strategies were applied to significantly improve enzyme potency and the polarity of the molecule was adjusted to gain cellular activity. The crystal structures of two representative inhibitors bound to Jak1 were obtained to enable SAR exploration.