Probing the stereoselectivity of P-glycoprotein—synthesis, biological activity and ligand docking studies of a set of enantiopure benzopyrano[3,4-b][1,4]oxazines
Chemical Communications2010Vol. 47(9), pp. 2586–2588
Citations Over TimeTop 23% of 2010 papers
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.
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