Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.

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Colabufo NA, Berardi F, Perrone R, Rapposelli S, Digiacomo M, Balsamo A

Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.

J Med Chem. 2006 Nov 2;49(22):6607-13.

PubMed ID

17064079 [ View in PubMed

]

Abstract

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Elacridar	P-glycoprotein 1	EC 50 (nM)	2000	N/A	N/A	Details
Verapamil	P-glycoprotein 1	EC 50 (nM)	20000	N/A	N/A	Details