CAM4066, a specific CK2α kinase inhibitor, is anchored in the cryptic αD pocket outside the active site and inserts a “warhead” into the active site, blocking ATP binding and thereby inhibiting the kinase.

Graphical abstract

We describe the development of a CAM4712, a novel CK2α inhibitor which does not interact with the ATP binding site and shows improved properties over the first-generation inhibitor CAM4066.

The asymmetric synthesis of helicenes … … by a Fischer indolization catalyzed by a SPINOL-derived phosphoric acid is reported by B. List et al. in their Communication on page 5202 ff. The catalyst is designed for long-range control and bears extended p-surfaces at the 3,3'-position. It creates a chiral nanometer-sized pocket, which enables p-p stacking interactions between the substituents and the reactive intermediate. A variety of (di)azahelicenes were obtained with good to excellent yields and enentioselectivities.