Synthesis and biological evaluation of novel 2(4’-hydroxynaphthyl)chromen-4-one as a CK2 inhibitor

Haidar S, Jabbour M, Al-Khayat MA, Aichele D, Jose J

Abstract

Protein kinase CK2 is a potential drug target for many diseases including cancer, inflammatory disorders, Alzheimer's disease, Parkinson's disease and viral infections. Significant efforts have been made for the discovery of potent inhibitors of this enzyme. Herein, we report on the synthesis, characterization, and biological evaluation of novel flavonoid compounds as CK2 inhibitors. The tested compounds were 2 (4`-hydroxynaphthyl) chromen-4-one which is a naphthyl backbone flavonoid with an IC50 value of 0.45±0.059 μM and 2(4-hydroxyphenyl)-4H-chromen-4-one a phenyl based derivative with an IC50 value of 0.33±0.048 μM. Cell viability was tested using MCF-7 cells. Both compounds were able to reduce the cell viability around 50 % in concentration of 100 μM after 48 h. Molecular modeling studies were performed to understand the binding mode of both compounds.