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Bis-pyranobenzoquinones as a new family of reversal agents of the multidrug resistance phenotype mediated by P-glycoprotein in mammalian cells and the protozoan parasite Leishmania

AuthorsJiménez-Alonso, S.; Pérez-Lomas, A. L.; Estévez-Braun, A.; Martínez, F. M.; Orellana, H. C.; Ravelo, Ángel G.; Gamarro, Francisco; Castanys, Santiago; López, Matías
Issue Date2008
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 51: 7132- 7143 (2008)
AbstractWe have synthesized a set of bis-pyranobenzoquinones through a direct and highly efficient approach based on a double intramolecular domino Knoevenagel hetero Diels-Alder reaction. These bis-pyranobenzoquinone derivatives are compounds whose skeletons have similarities to those of some anticancerous and leishmanicidal drugs. Considering that these drugs are substrates for some members of the ATP-binding cassette (ABC) family of proteins that confers a multidrug resistance (MDR) phenotype, we have carried out the biological evaluation of 20 bis-pyranobenzoquinones as modulators of the MDR phenotype in mammalian cell lines overexpressing P-glycoprotein, MRP1, or BCRP. Moreover, we also tested some of these compounds as potential MDR modulators in a Leishmania tropica line overexpressing a P-glycoprotein-like transporter. Compounds 9 and 10 are, in this work, the most promising reversal agents of MDR in human cancer cell lines, while compounds 4 and 20 showed potent reversal activity of MDR phenotype in the protozoan parasite Leishmania. © 2008 American Chemical Society.
Identifiersdoi: 10.1021/jm800403b
issn: 0022-2623
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