Abstract : Iodinated derivatives of verapamil were synthesized and tested as P-glycoprotein (Pgp)-mediated multidrug resistance (MDR) reversal agents. The ability of these compounds to revert MDR was evaluated on daunorubicin-resistant K562 cells, by measuring the intracellular accumulation of rhodamine 123, a fluorescent probe of Pgp transport activity. One of the investigated compounds (16c) was found to be a more potent MDR reversal agent than verapamil and cyclosporin A, used as reference molecules. Further in vitro studies showed that compound 16c restored daunorubicin activity and, when used alone, did not induce cell death, cell cycle perturbation and modification of calcium channel activity in comparison with verapamil.
Type de document :
Article dans une revue
Anticancer Research, International Institute of Anticancer Research, 2010, 30 (7), pp.2553-9
http://www.hal.inserm.fr/inserm-00520132
Contributeur : Marco Canepari
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Soumis le : mercredi 22 septembre 2010 - 12:04:43
Dernière modification le : vendredi 13 avril 2018 - 16:44:34
Document(s) archivé(s) le : vendredi 2 décembre 2016 - 03:57:13
Régis Barattin, Bastien Gerby, Kevin Bourges, Gaëlle Hardy, Jose Olivares, et al.. Iodination increases the activity of verapamil derivatives in reversing PGP multidrug resistance.. Anticancer Research, International Institute of Anticancer Research, 2010, 30 (7), pp.2553-9. 〈inserm-00520132〉
