Abstract
Optimization of pyrazinoindolone inhibitors of MAPKAP-K2 (MK2) provides a reasonable balance of cellular potency and physicochemical properties. Mechanistic studies support the inhibition of MK2 which is responsible for the sub-micromolar cellular efficacy.
MeSH terms
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Combinatorial Chemistry Techniques*
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / chemistry
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Enzyme Inhibitors / pharmacology*
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Indoles / chemical synthesis*
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Indoles / chemistry
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Indoles / pharmacology*
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Inhibitory Concentration 50
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Intracellular Signaling Peptides and Proteins / antagonists & inhibitors*
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Molecular Structure
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Protein Serine-Threonine Kinases / antagonists & inhibitors*
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Pyrazoles / chemical synthesis*
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Pyrazoles / chemistry
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Pyrazoles / pharmacology*
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Indoles
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Intracellular Signaling Peptides and Proteins
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Pyrazoles
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MAP-kinase-activated kinase 2
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Protein Serine-Threonine Kinases