The growing impact of click chemistry on drug discovery

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Click chemistry is a modular approach that uses only the most practical and reliable chemical transformations. Its applications are increasingly found in all aspects of drug discovery, ranging from lead finding through combinatorial chemistry and target-templated in situ chemistry, to proteomics and DNA research, using bioconjugation reactions.

In this article Hartmuth C. Kolb and K. Barry Sharpless discuss drug discovery approaches based on the copper-(I)-catalyzed formation of triazoles from azides and acetylenes. They discuss how this triazole-forming process, and click chemistry in general, promise to accelerate both lead finding and lead optimization, due, above all, to its great scope, modular design, and reliance.

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