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In addition to P-glycoprotein/ABCB 1,for which third-generation inhibitors are in clinical development,two more-recently discovered ABC (ATP-binding cassette) transporters are critically involved in tumor resistance to anticancer drugs:breast cancer resistance protein/ABCG2 and multidrug resistance protein/ABCC1.Screening of various classes of flavonoids as inhibitors ofmitoxantrone efflux from ABCG2-transfected HEK293 cells by flow cytometry,and as chemosensitizers of cell proliferation,allowed to establish 3D Quantitative Structure-Activity Relationships.