A series of 4, 6-dimethoxyaurones were synthesized by reacting 4, 6-dimethoxybenzofuran- 3 (2H)-one with various benzaldehydes in a base-catalyzed aldol reaction. AZ configuration was assigned to the aurones based on spectroscopic and crystallographic data. The aurones were tested for their ability to modulate ABCG2 (breast cancer resistance protein)- mediated multidrug resistance in vitro. Several members (0.5 μM) increased the ...