Abstract

Remember the enediynes? These bacterial natural products, first isolated in the 1960s, were found to have powerful antibiotic and anticancer properties. In the late 1980s and early '90s, they generated intense research interest as organic chemists competed to be first to synthesize them and drug companies pursued potential enediyne drugs. Enediynes initially proved to be problematic drug candidates, due in part to their high toxicity, and in recent years interest may seem to have faded. But enediyne research has indeed continued to perk quietly along, and several lines of investigation are now coming to fruition: The production genes for two enediynes have just been identified, a new resistance protein (a protein that protects a producing organism from its own enediyne) has been found, enediyne clinical trials are being carried out, and an enediyne-based antibody conjugate is currently up for marketing approval. The shared feature of all enediyne compounds is their enediyne chemical group—a large carbon ...

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