Design and development of 9,10-dihydrophenanthrene derivatives as inhibitors of human protein kinase CK2

Haidar S, Aichele D, Popp R, Meyers A, Jose J

Abstract

Protein kinase CK2 is an emerging target for the therapeutic intervention in human diseases, particularly in cancer. Inhibitors of this enzyme are currently in clinical trials, indicating thedruggability of human CK2. Here we report on the design of several derivatives of 9,10-Dihydrophenanthrene with di-substituted functional groups, using a molecular modeling approach.The inhibitory activity of the synthesized compounds towards CK2 was tested using a capillary electrophoresis in-vitro approach. Furthermore, breast cancer cells (MCF-7) were treatedwith the designed compounds and cell viability was determined using the MTT assay. Molecular modeling studies were performed using MOE software to understand the binding affinitiesof the designed compounds