Potent and Selective Inhibitors of CK2 Kinase Identified through Structure-Guided Hybridization

Abstract

In this paper we describe a series of 3-cyano-5-aryl-7-aminopyrazolo­[1,5-<i>a</i>]­pyrimidine hits identified by kinase-focused subset screening as starting points for the structure-based design of conformationally constrained 6-acetamido-indole inhibitors of CK2. The synthesis, SAR, and effects of this novel series on Akt signaling and cell proliferation <i>in vitro</i> are described