The Application of Diversity oriented Synthesis in Chemical Biology

Communicable and non-communicable diseases are prevalent worldwide. Whilst treatments and cures exist for several of these, for many more they are either ineffective or non-existent. Cancer, malaria and antibiotic resistance are some representative examples of conditions that cause huge burdens on worldwide healthcare. However, despite research and development investment being higher than ever, the biomedical community struggles to provide effective solutions for such devastating diseases. This can be attributed to the inability to identify appropriate targets to modulate the disease, the lack of suitable compounds to interact with identified targets, or the failure of compounds to pass through clinical trials. In such a situation, the question remains as to where the problem fundamentally lies and how to address it. This chapter will analyse the importance of screening high-quality small-molecule collections to facilitate the identification of novel biologically-active small molecules and how different diversity-oriented synthesis (DOS) approaches have efficiently addressed this issue.