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The discovery of tricyclic pyridone JAK2 inhibitors. Part 1: hit to lead |
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| Authors: | 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 |
| Affiliation: | Department of Chemistry, Merck & Co., Boston, MA 02115, USA. tony_siu@merck.com |
| 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 log D. These efforts led to the identification of compound 41, which demonstrates in vivo activity in our study. |
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| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |