Synthesis and Biological
Evaluation of Neopeltolide and Analogs
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Abstract
The synthesis of neopeltolide analogues that contain
variations in the oxazole-containing side chain and in the macrolide
core are reported along with the GI<sub>50</sub> values for these
compounds against MCF-7, HCT-116, and p53 knockout HCT-116 cell lines.
Although biological activity is sensitive to changes in the macrocycle
and the side chain, several analogues displayed GI<sub>50</sub> values
of <25 nM. Neopeltolide and several of the more potent analogues
were significantly less potent against p53 knockout cells, suggesting
that p53 plays an auxiliary role in the activity of these compounds
