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Article

Synthesis, cellular evaluation, and mechanism of action of piperlongumine analogs.

Proceedings of the National Academy of Sciences of the United States of America - 18 Sept 2012

Adams Drew J, Dai Mingji, Pellegrino Giovanni, Wagner Bridget K, Stern Andrew M, Shamji Alykhan F, Schreiber Stuart L

Abstract excerpt

Piperlongumine is a naturally occurring small molecule recently identified to be toxic selectively to cancer cells in vitro and in vivo. This compound was found to elevate cellular levels of reactive oxygen species (ROS) selectively in cancer cell lines. The synthesis of 80 piperlongumine analogs has revealed structural modifications that retain, enhance, and ablate key piperlongumine-associated effects on cells,...

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Identifiers

PMID: 22949699
DOI: 10.1073/pnas.1212802109
PMCID: PMC3458345

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