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PDBsum entry 5cxh
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Transferase/transferase inhibitor
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PDB id
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5cxh
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References listed in PDB file
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Key reference
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Title
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Orally bioavailable syk inhibitors with activity in a rat pk/pd model.
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Authors
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G.Thoma,
S.Veenstra,
R.Strang,
J.Blanz,
E.Vangrevelinghe,
J.Berghausen,
C.C.Lee,
H.G.Zerwes.
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Ref.
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Bioorg Med Chem Lett, 2015,
25,
4642-4647.
[DOI no: ]
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PubMed id
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Abstract
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Design and optimization of benzo- and pyrido-thiazoles/isothiazoles are reported
leading to the discovery of the potent, orally bioavailable Syk inhibitor 5,
which was found to be active in a rat PK/PD model. Compound 5 showed acceptable
overall kinase selectivity. However, in addition to Syk it also inhibited Aurora
kinase in enzymatic and cellular settings leading to findings in the
micronucleus assay. As a consequence, compound 5 was not further pursued.
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