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Synthesis and biological evaluation of neopeltolide and analogs.

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(50) 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(50) 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.

SUBMITTER: Cui Y

PROVIDER: S-EPMC3308185 | biostudies-literature | 2012 Mar

REPOSITORIES: biostudies-literature

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Synthesis and biological evaluation of neopeltolide and analogs.

Cui Yubo Y Balachandran Raghavan R Day Billy W BW Floreancig Paul E PE

The Journal of organic chemistry 20120222 5

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(50) 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(50) values of <25 nM. Neopeltolide and several of the more potent analogues were significantly less potent against p53 knockout ...[more]

PMID: 22329423

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