Design and synthesis of a novel class of CK2 inhibitors: application of copper- and gold-catalysed cascade reactions for fused nitrogen heterocycles.

Two classes of fused nitrogen heterocycles were designed as CK2 inhibitor candidates on the basis of previous structure-activity relationship (SAR) studies. Various dipyrrolo[3, 2-b:2', 3'-e]pyridine and benzo[g]indazole derivatives were prepared using transition-metal-catalysed cascade and/or multicomponent reactions. Biological evaluation of these candidates revealed that benzo[g]indazole is a promising scaffold for potent CK2 inhibitors. The inhibitory activities on cell proliferation of these potent CK2 inhibitors are also presented

Intramolecular Base-Accelerated Radical-Scavenging Reaction of a Planar Catechin Derivative Bearing a Lysine Moiety

A planar catechin derivatives incorporating a lysine moiety was synthesized and showed ~400-fold increased radical-scavenging activity relative to naturally-occurring (+)-catechin