The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: Hit to lead

…, ES Kozina, J Jung, C Rosenstein, A Mathur…

Index: Siu, Tony; Kozina, Ekaterina S.; Jung, Joon; Rosenstein, Craig; Mathur, Anjili; Altman, Michael D.; Chan, Grace; Xu, Lin; Bachman, Eric; Mo, Jan-Rung; Bouthillette, Melaney; Rush, Thomas; Dinsmore, Christopher J.; Marshall, C. Gary; Young, Jonathan R. Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 24 p. 7421 - 7425

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Citation Number: 17

Abstract

This paper describes the discovery and design of a novel class of JAK2 inhibitors. Furthermore, we detail the optimization of a screening hit using ligand binding efficiency and logD. These efforts led to the identification of compound 41, which demonstrates in vivo activity in our study.