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1.0 Introduction
1.1 The Role of Diversity-Oriented Synthesis in Modern Biomedical Research
Modern drug discovery efforts are based upon a deep understanding of the cellular
pathways responsible for a particular disease. The extreme complexity of the cellular circuitry
has made the goal of understanding all of its aspects a formidable challenge. Significant progress
in this area has been made by using modern biochemical tools such as mutagenesis, which is
commonly used to irreversibly modify proteins in order to understand their cellular function.
However, there are many aspects of the cell’s biochemistry that remain a mystery. These include
important signaling pathways based on dynamic protein-protein interactions that are particularly
difficult to study. 1 Therefore, there is a tremendous need for innovative strategies to discover
new cellular pathways and probe the function of various protein targets.
Small organic molecules are useful research probes for studying cellular pathways. Small
molecules are capable of interacting with macromolecules such as proteins generally in a
reversible manner, thereby modulating their function. 2 Observing the effects that result from
such interactions in designed assays can often lead to an understanding of the role a particular
target plays in the cell. Additionally, if the protein is a known therapeutically relevant target, lead
compounds for drug discovery can be identified. The great number of relevant protein targets
and their immense structural diversity dictates that the small molecules screened against these
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