Journal of Medicinal Chemistry p. 1950 - 1963 (2015)
Update date:2022-08-15
Topics:
Thoma, Gebhard
Smith, Alexander B.
Van Eis, Maurice J.
Vangrevelinghe, Eric
Blanz, Joachim
Aichholz, Reiner
Littlewood-Evans, Amanda
Lee, Christian C.
Liu, Hong
Zerwes, Hans-Günter
We describe the discovery of selective and potent Syk inhibitor 11, which exhibited favorable PK profiles in rat and dog and was found to be active in a collagen-induced arthritis model in rats. Compound 11 was selected for further profiling, but, unfortunately, in GLP toxicological studies it showed liver findings in rat and dog. Nevertheless, 11 could become a valuable tool compound to investigate the rich biology of Syk in vitro and in vivo.
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(2020)