A novel class of molecules with structure N-（3-arylpropyl）-9,10-dihydro-9-oxoacridine-4-carboxamides （20- 29） were designed by generating a pharmacophore for potent MDR reversal activity using phase drug design so...A novel class of molecules with structure N-（3-arylpropyl）-9,10-dihydro-9-oxoacridine-4-carboxamides （20- 29） were designed by generating a pharmacophore for potent MDR reversal activity using phase drug design software. The designed molecules were synthesized by a novel synthesis route and evaluated for their inhibitory effects on the transport activity of P-glycoprotein （P-gp） by standard Hoechst 33342 assay method. Based on the pIC50 values of ten title compounds screened, three compounds exhibited better activity as compared to Verapamil used as standard.展开更多
文摘A novel class of molecules with structure N-（3-arylpropyl）-9,10-dihydro-9-oxoacridine-4-carboxamides （20- 29） were designed by generating a pharmacophore for potent MDR reversal activity using phase drug design software. The designed molecules were synthesized by a novel synthesis route and evaluated for their inhibitory effects on the transport activity of P-glycoprotein （P-gp） by standard Hoechst 33342 assay method. Based on the pIC50 values of ten title compounds screened, three compounds exhibited better activity as compared to Verapamil used as standard.
