4.8 Article

Nocardioazines: A Novel Bridged Diketopiperazine Scaffold from a Marine-Derived Bacterium Inhibits P-Glycoprotein

Journal

ORGANIC LETTERS
Volume 13, Issue 10, Pages 2770-2773

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol200904v

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Funding

  1. Australian Postgraduate Award
  2. University of Queensland
  3. Australian Research Council, UQ [LP0989954]
  4. Institute for Molecular Bioscience
  5. Australian Research Council [LP0989954] Funding Source: Australian Research Council

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An Australian marine sediment-derived Isolate, Nocardiopsis sp. (CMB-M0232), yielded a new class of prenylated diketopiperazine, Indicative of the action of a uniquely regioselective diketopiperazine indole prenyltransferase. The bridged scaffold of nocardioazine A proved to be a noncytotoxic inhibitor of the membrane protein efflux pump P-glycoprotein, reversing doxorubicin resistance in a multidrug resistant colon cancer cell.

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