A facile synthesis and biological activity of novel tetrahydrobenzo[4′,5′]thieno[3′,2′:5,6]pyrido[4,3- d]pyrimidin-4(3 H)-ones

Abstract

The synthesis and biological activity of 2-substituted-8,9,10,11-tetrahydrobenzo[4′,5′]thieno[3′,2′:5,6] pyrido[4,3- d]pyrimidin-4(3 H)-ones are described. Bioassay results indicated that these compounds have antifungal activity against Botrytis cinerea at a concentration of 50 mg/L. In addition, compounds 5m and 5n were effective to both KB cells and their parent multidrug resistant KBv200 cells with the overexpression of ABCB1. For example, compound 5m showed the best inhibition against KB and KBv200 cells with IC 50 values of 17.4 and 25.4 μM, respectively.