Abstract

Abstract The design and synthesis of enantiomerically enriched hybrid molecules, 1a–c and 2a–c , have been accomplished by employing the lipase-mediated asymmetric acetylation of prochiral diol 9 as the key step. Evaluation of their DNA-cleaving activity has revealed the unnatural type of enantiomer 2a-c to be more potent than 1a-c with natural configuration.

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