Abstract
The synthesis of new “selectively activated” enediyne prodrugs is reported. These compounds, belonging to the “lactenediyne” family, each possess a protected primary amine tethered at the β-lactam nitrogen. This, once deblocked, can act as a trigger, provoking a cascade of events probably terminating with Bergman cycloaromatization of the enediyne moiety. In vitro experiments on plasmid DNA have shown that the protected compounds are inactive, while the unprotected amine is able to provoke single-strand scissions. These results open the way towards development of enzymatically activated lactenediyne prodrugs. (© Wiley-VCH Verlag GmbH, 69451 Weinheim, Germany, 2002)
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