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Publication Abstract from PubMed
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.
Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors.,Padilla F, Bhagirath N, Chen S, Chiao E, Goldstein DM, Hermann JC, Hsu J, Kennedy-Smith JJ, Kuglstatter A, Liao C, Liu W, Lowrie LE Jr, Luk KC, Lynch SM, Menke J, Niu L, Owens TD, O-Yang C, Railkar A, Schoenfeld RC, Slade M, Steiner S, Tan YC, Villasenor AG, Wang C, Wanner J, Xie W, Xu D, Zhang X, Zhou M, Lucas MC J Med Chem. 2013 Feb 28;56(4):1677-92. doi: 10.1021/jm301720p. Epub 2013 Feb 12. PMID:23350847[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
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References
- ↑ Padilla F, Bhagirath N, Chen S, Chiao E, Goldstein DM, Hermann JC, Hsu J, Kennedy-Smith JJ, Kuglstatter A, Liao C, Liu W, Lowrie LE Jr, Luk KC, Lynch SM, Menke J, Niu L, Owens TD, O-Yang C, Railkar A, Schoenfeld RC, Slade M, Steiner S, Tan YC, Villasenor AG, Wang C, Wanner J, Xie W, Xu D, Zhang X, Zhou M, Lucas MC. Pyrrolopyrazines as selective spleen tyrosine kinase inhibitors. J Med Chem. 2013 Feb 28;56(4):1677-92. doi: 10.1021/jm301720p. Epub 2013 Feb 12. PMID:23350847 doi:http://dx.doi.org/10.1021/jm301720p
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