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Finding cures for cancer, AIDS, and the plethora of other ailments that plague humans conjures up images from the 1992 movie Medicine Man. In it, Sean Connery as Dr. Robert Campbell treks through the tropical Amazon forests searching for an enigmatic plant that seems to produce a cancer-curing compound. Although scientists may never approach Mother Nature's ability to create novel compounds, new combinatorial chemistry techniques make a very respectable effort. Multitudes of new compounds can be synthesized rapidly, and high-throughput screening technology provides a mechanism to test them for beneficial properties. In fact, it can be argued that combinatorial chemistry provides the first real opportunity to capitalize on high-throughput screening.

In some ways, combinatorial chemistry is to modern drug development what PCR was to molecular biology. In the past, drug development entailed the design and synthesis of individual compounds to target...

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