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Issue 9, 2011
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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

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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.

Graphical abstract: 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

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Article information


Submitted
05 Aug 2010
Accepted
24 Nov 2010
First published
21 Dec 2010

Chem. Commun., 2011,47, 2586-2588
Article type
Communication

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

I. Jabeen, P. Wetwitayaklung, F. Klepsch, Z. Parveen, P. Chiba and G. F. Ecker, Chem. Commun., 2011, 47, 2586 DOI: 10.1039/C0CC03075A

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