Exploring and exploiting biologically relevant chemical space.

Small bioactive molecules are pre-requisite for any discovery discipline. Aware of the fact that bioactivity is not randomly dispersed in the vast chemical space, chemists have been developing hypothesis that can lead them to the islands of bioactivities. Natural products have always been a source of inspiration and their structural motifs provide biologically relevant starting points for library synthesis. In addition to that, Diversity Oriented Synthesis (DOS) and Biology Oriented Synthesis (BIOS) have emerged as tools to guide synthesis design and help enrich compound collections in biological activities. Coherent developments in chem- and bioinformatic tools and in organic synthesis methods targeting efficient generation of compound collections are required to identify interesting molecules that can be employed as chemical probes in chemical biology research and drug candidates in medicinal chemistry investigations.