Abstract
A series of hybrid molecules consisting of benzophenones and N-cyclopropyl-3-methylbenzamides were synthesized and biologically evaluated as novel p38 mitogen activated protein kinase (MAPK) inhibitors. In particular, we found that compound 10g displayed potent p38α MAPK inhibitory activity (IC50=0.027 μM), high kinase selectivity, and significant anti-inflammatory activity in THP-1 monocyte cells.
Keywords:
Benzophenone; Hybrid; Kinase selectivity; N-Cyclopropylbenzamide; P38 mitogen activated protein kinase inhibitor.
Copyright © 2015 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Benzamides / chemistry
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Benzophenones / chemistry*
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Cell Line / drug effects
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Chemistry Techniques, Synthetic
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Drug Design
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Drug Evaluation, Preclinical / methods
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Humans
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Inhibitory Concentration 50
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Monocytes / drug effects
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / pharmacology*
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Structure-Activity Relationship
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p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
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p38 Mitogen-Activated Protein Kinases / chemistry
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p38 Mitogen-Activated Protein Kinases / metabolism
Substances
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Anti-Inflammatory Agents, Non-Steroidal
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Benzamides
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Benzophenones
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Protein Kinase Inhibitors
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benzophenone
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p38 Mitogen-Activated Protein Kinases