Pyrrolopyrazines as Selective Spleen Tyrosine Kinase Inhibitors
Journal of Medicinal Chemistry2013Vol. 56(4), pp. 1677–1692
Citations Over TimeTop 10% of 2013 papers
Fernando Padilla, Niala Bhagirath, Shaoqing Chen, Eric Chiao, David Goldstein, Johannes C. Hermann, Jonathan C. Hsu, Joshua J. Kennedy‐Smith, A. Kuglstatter, Cheng Liao, Wenjian Liu, Lee Lowrie, Kin Chun Luk, Stephen M. Lynch, John G. Menke, Linghao Niu, Timothy D. Owens, Counde O-Yang, Aruna Railkar, Ryan C. Schoenfeld, Michelle Slade, Sandra Steiner, Yun-Chou Tan, Armando G. Villaseñor, Ce Wang, Jutta Wanner, Wenwei Xie, Daigen Xu, Xiaohu Zhang, Mingyan Zhou, Matthew C. Lucas
Abstract
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.
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