Chemical compounds isolated from natural sources offer unique opportunities to understand life on a molecular level. In this account, an overview over different natural products investigated in our research group over the last decade is presented. We have shown that protein localization in living cells can be controlled by anguinomycins and derivatives. Furthermore, a truncated analog, SB640, was discovered that retained much of the natural product potency. Detailed studies of the iron chelator anachelin led to the development of a bio-inspired platform for the generation of bioactive interfaces. The discovery of natural products isolated from cyanobacteria such as nostocarboline, aerucyclamides, cyanopetolin 1020 and various microcystins is presented and their molecular mechanisms of action were investigated. The last part describes the synthesis and evaluation of various natural products involved in neuritogenesis and synapse reconstruction such as withanolide A, militarinone, farinosone A and C and torrubiellone C. Their potential with regard to their use in regenerative medicine is discussed.