Abstract
Syntheses of 16-membered macrolactams, which were aza-analogues of macrosphelides, could be established effectively by a ring-closing metathesis (RCM) strategy. Novel 19 analogues and six aza-macrosphelide–epothilone hybrids were furnished according to simple operations. Biological assay of these artificial aza-macrosphelides revealed that some of them showed stronger apoptosis-inducing activity against human lymphoma cells than the parent compound.
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