Is synthesis the main hurdle for the generation of diversity in compound libraries for screening?

BACKGROUND 'Diversity' is often cited as a crucial consideration when generating compound collections for biological screening. However, what exactly does one mean by 'diversity' and why is it important? OBJECTIVE How can diversity be incorporated into compound collections and what are the theoretical and technical challenges this poses? In this editorial, we comment on various factors involved in the creation of structurally, and most crucially, functionally diverse compound libraries. CONCLUSIONS In particular, we highlight the central role played by organic synthesis and discuss the value of diversity-driven synthetic approaches in the search for new biologically active molecules with potentially exciting and unusual biological properties.