Abstract

\beta-lactam fused enediynes have been successfully synthesized by intramolecular Kinugasa reaction in moderate yields.
DSC studies indicated significant influence of the \beta-lactam ring upon the reactivity of enediynes. None of the \beta-lactam
fused enediynes (under ring opening conditions) as well as the 11-membered monocyclic enediyne as the tosylate salt
showed any cleavage of plasmid DNA. Interestingly, the 10-membered enediyne as the tosylate salt cleaved both single
and double strands of plasmid DNA at micromolar concentration.

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