Structure–activity relationship study of EphB3 receptor tyrosine kinase inhibitors

L Qiao, S Choi, A Case, TG Gainer, K Seyb…

Index: Qiao, Lixin; Choi, Sungwoon; Case, April; Gainer, Thomas G.; Seyb, Kathleen; Glicksman, Marcie A.; Lo, Donald C.; Stein, Ross L.; Cuny, Gregory D. Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 21 p. 6122 - 6126

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Citation Number: 18

Abstract

A structure–activity relationship study for a 2-chloroanilide derivative of pyrazolo [1, 5-a] pyridine revealed that increased EphB3 kinase inhibitory activity could be accomplished by retaining the 2-chloroanilide and introducing a phenyl or small electron donating substituents to the 5-position of the pyrazolo [1, 5-a] pyridine. In addition, replacement of the pyrazolo [1, 5-a] pyridine with imidazo [1, 2-a] pyridine was well tolerated and resulted in ...