Journal of medicinal chemistry, 2013-02, Vol.56 (4), p.1677-1692
- Padilla, Fernando
- Bhagirath, Niala
- Chen, Shaoqing
- Chiao, Eric
- Goldstein, David M
- Hermann, Johannes C
- Hsu, Jonathan
- Kennedy-Smith, Joshua J
- Kuglstatter, Andreas
- Liao, Cheng
- Liu, Wenjian
- Lowrie, Lee E
- Luk, Kin Chun
- Lynch, Stephen M
- Menke, John
- Niu, Linghao
- Owens, Timothy D
- O-Yang, Counde
- Railkar, Aruna
- Schoenfeld, Ryan C
- Slade, Michelle
- Steiner, Sandra
- Tan, Yun-Chou
- Villaseñor, Armando G
- Wang, Ce
- Wanner, Jutta
- Xie, Wenwei
- Xu, Daigen
- Zhang, Xiaohu
- Zhou, Mingyan
- Lucas, Matthew C
2013
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- Autor(en) / Beteiligte
- Padilla, Fernando
- Bhagirath, Niala
- Chen, Shaoqing
- Chiao, Eric
- Goldstein, David M
- Hermann, Johannes C
- Hsu, Jonathan
- Kennedy-Smith, Joshua J
- Kuglstatter, Andreas
- Liao, Cheng
- Liu, Wenjian
- Lowrie, Lee E
- Luk, Kin Chun
- Lynch, Stephen M
- Menke, John
- Niu, Linghao
- Owens, Timothy D
- O-Yang, Counde
- Railkar, Aruna
- Schoenfeld, Ryan C
- Slade, Michelle
- Steiner, Sandra
- Tan, Yun-Chou
- Villaseñor, Armando G
- Wang, Ce
- Wanner, Jutta
- Xie, Wenwei
- Xu, Daigen
- Zhang, Xiaohu
- Zhou, Mingyan
- Lucas, Matthew C
- Titel
- Pyrrolopyrazines as Selective Spleen Tyrosine Kinase Inhibitors
- Ist Teil von
- Journal of medicinal chemistry, 2013-02, Vol.56 (4), p.1677-1692
- Ort / Verlag
- United States: American Chemical Society
- Erscheinungsjahr
- 2013
- Quelle
- MEDLINE
- Beschreibungen/Notizen
- We describe the discovery of several pyrrolopyrazines as potent and selective Syk inhibitors and the efforts that eventually led to the desired improvements in physicochemical properties and human whole blood potencies. Ultimately, our mouse model revealed unexpected toxicity that precluded us from further advancing this series.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0022-2623eISSN: 1520-4804DOI: 10.1021/jm301720pTitel-ID: cdi_crossref_primary_10_1021_jm301720p
- Format
- –
- Schlagworte
- Animals, B-Lymphocytes - drug effects, B-Lymphocytes - enzymology, Blood Proteins - metabolism, Crystallography, X-Ray, Humans, Intracellular Signaling Peptides and Proteins - antagonists & inhibitors, Mice, Microsomes, Liver - metabolism, Models, Molecular, Molecular Structure, Protein Binding, Protein-Tyrosine Kinases - antagonists & inhibitors, Pyrazines - chemical synthesis, Pyrazines - pharmacology, Pyrazines - toxicity, Pyrroles - chemical synthesis, Pyrroles - pharmacology, Pyrroles - toxicity, Structure-Activity Relationship, Syk Kinase