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Arylmethyloxyphenyl derivatives: small molecules displaying P-glycoprotein inhibition.

作者信息

Colabufo Nicola Antonio, Berardi Francesco, Perrone Roberto, Rapposelli Simona, Digiacomo Maria, Balsamo Aldo

机构信息

Dipartimento Farmacochimico, Università degli Studi di Bari, Via Orabona 4, 70125 Bari, Italy.

出版信息

J Med Chem. 2006 Nov 2;49(22):6607-13. doi: 10.1021/jm060639z.

DOI:10.1021/jm060639z
PMID:17064079
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.

摘要

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