Abstract
A series of enantiomerically pure benzopyrano[3,4-b][1,4]oxazines have been synthesised and tested for their ability to inhibit P-glycoprotein. Reducing the conformational flexibility of the molecules leads to remarkable differences in the activity of diastereoisomers. Docking studies into a homology model of human P-gp provide first insights into potential binding areas for these compounds.
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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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Benzopyrans / chemistry*
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Binding Sites
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Computer Simulation
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Ligands
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Oxazines / chemistry*
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Rhodamines / chemistry
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Stereoisomerism
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Benzopyrans
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Ligands
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Oxazines
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Rhodamines