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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 

Arylmethyloxyphenyl derivatives: small molecules displaying p-glycoprotein inhibition.

Some arylmethyloxyphenyl derivatives were prepared as simplified structures of analogous arylpiperazines with high affinity toward dopaminergic D(2) and serotonergic 5-HT(1A) receptors and inhibiting P-glycoprotein (P-gp). The compounds 5b and 8b displayed good P-gp inhibition activity measured as [(3)H]vinblastine transport inhibition in the Caco-2 cell monolayer and intracellular doxorubicin accumulation in MCF7/Adr cells by flow cytometry. Compounds 5b and 8b also inhibited, dose-dependently, ATP-ase activation induced by P-gp substrate vinblastine.[1]

References

  1. Arylmethyloxyphenyl derivatives: small molecules displaying p-glycoprotein inhibition. Colabufo, N.A., Berardi, F., Perrone, R., Rapposelli, S., Digiacomo, M., Balsamo, A. J. Med. Chem. (2006) [Pubmed]
 
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