The presentation will illustrate how the structural properties of metal complexes can be applied to the design of molecules with unprecedented biological properties. For example, recent results from our laboratory demonstrate that organometallic compounds can function as highly potent and selective enzyme inhibitors. Along these lines, a recipe is introduced for morphing indolocarbazole alkaloids into simple and easily accessible metal complexes, leading to the discovery of picomolar and maybe even femtomolar inhibitors for protein kinases. Some of these compounds display promising anticancer properties.