1,4-Benzodiazepin-2-ones have applications in many areas of medicinal chemistry that are not restricted to 'classical' CNS treatments such as sedatives, epilepsy and muscle relaxants. We will describe selected examples of 1,4-benzodiazepin-2-ones in other areas of medicinal chemistry including uses as G-protein-coupled receptor antagonists, enzyme inhibitors and anticancer agents. Examples from our group will mainly show the use of palladacycle complexes of 1,4-benzodiazepin-2-ones as anticancer agents.