Abstract
We designed and synthesized conformationally restricted analogues and regioisomers of the nonsteroidal anti-inflammatory drug indomethacin. Evaluation of the inhibitory effects of these compounds on COX, P-glycoprotein, and multidrug resistance indicated that NSAIDS modulation of multidrug-resistant P-glycoprotein and multidrug-resistant protein-1 is not associated with COX-1 and COX-2 inhibitory activities.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
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Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
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Anti-Inflammatory Agents, Non-Steroidal / chemistry
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Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
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Cell Line, Tumor
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Chemistry Techniques, Synthetic
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Cyclooxygenase Inhibitors / chemical synthesis
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Cyclooxygenase Inhibitors / chemistry
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Cyclooxygenase Inhibitors / pharmacology
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Drug Design*
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Drug Resistance, Multiple / drug effects
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Humans
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Indomethacin / analogs & derivatives
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Indomethacin / chemical synthesis*
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Indomethacin / chemistry
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Indomethacin / pharmacology*
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Models, Molecular
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Molecular Conformation
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Prostaglandin-Endoperoxide Synthases / metabolism
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Anti-Inflammatory Agents, Non-Steroidal
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Cyclooxygenase Inhibitors
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Prostaglandin-Endoperoxide Synthases
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Indomethacin