期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 21, 页码 5923-5930出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.08.082
关键词
JAK inhibitors; 8-Oxo-pyridopyrimidines; Rheumatoid arthritis; Hematopoiesis
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. (C) 2013 Published by Elsevier Ltd.
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