Abstract
The p38 mitogen-activated protein kinase inhibitor VX-745 is prepared rapidly and efficiently in a four-step sequence using a combination of conductive heating and microwave-mediated steps. Its inhibitory activity was confirmed in hTERT immortalized HCA2 and WS dermal fibroblasts at 0.5-1.0 microM concentration by ELISA and immunoblot assay, and displays excellent kinase selectivity over the related stress-activated kinase JNK.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Blotting, Western
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Enzyme-Linked Immunosorbent Assay
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Protein Kinase Inhibitors / pharmacology*
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Pyridazines / chemical synthesis*
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Pyridazines / pharmacology
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Pyrimidines / chemical synthesis*
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Pyrimidines / pharmacology
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Werner Syndrome / enzymology*
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Werner Syndrome / pathology
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p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
Substances
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Protein Kinase Inhibitors
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Pyridazines
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Pyrimidines
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p38 Mitogen-Activated Protein Kinases
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VX-745