Design, synthesis and bioactivity study on 5-phenylfuran derivatives as potent reversal agents against P-glycoprotein-mediated multidrug resistance in MCF-7/ADR cell

P-glycoprotein (P-gp)-mediated multidrug resistance (MDR) is a phenomenon in which cells become resistant to structurally and mechanistically unrelated drugs resulting low intracellular drug concentrations. It one of the noteworthy problems malignant tumor clinical therapeutics. So P-gp protein ideal targets solve MDR. Based on lead compound 5m obtained from our previous work, series furan derivatives featuring alkyl-substituted phenols 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline were designed synthesized as reversal agents against this paper. Compound 16 containing isopropoxy possessed good potency mediated MDR MCF-7/ADR (IC50 (doxorubicin) = 0.73 ?M, RF 69.6 with 5 ?M treated). Western blot results Rh123 accumulation assays showed that effectively inhibited efflux function but not its expression. The preliminary structure–activity relationship docking studies demonstrated would be potential inhibitor. Most worthy mention has achieved satisfactory combination variety anti-tumor drugs, such doxorubicin, paclitaxel, vincristine. This study forwards hopeful inhibitor for withstanding cell setting basis further studies.