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Cryptocaryols A-H, alpha-Pyrone-Containing 1,3-Polyols from Cryptocarya sp Implicated in Stabilizing the Tumor Suppressor Pdcd4

  1. Author:
    Grkovic, T.
    Blees, J. S.
    Colburn, N. H.
    Schmid, T.
    Thomas, C. L.
    Henrich, C. J.
    McMahon, J. B.
    Gustafson, K. R.
  2. Author Address

    [Grkovic, T; Thomas, CL; Henrich, CJ; McMahon, JB; Gustafson, KR] NCI, Mol Targets Lab, Ctr Canc Res, Frederick, MD 21702 USA [Blees, JS; Colburn, NH] NCI, Lab Canc Prevent, Ctr Canc Res, Frederick, MD 21702 USA [Blees, JS; Schmid, T] Goethe Univ Frankfurt, Inst Biochem 1, Fac Med, D-60590 Frankfurt, Germany [Henrich, CJ] NCI, SAIC Frederick, Frederick, MD 21702 USA;Gustafson, KR (reprint author), NCI, Mol Targets Lab, Ctr Canc Res, Frederick, MD 21702 USA;gustafki@mail.nih.gov
    1. Year: 2011
    2. Date: May
  1. Journal: Journal of Natural Products
    1. 74
    2. 5
    3. Pages: 1015-1020
  2. Type of Article: Article
  3. ISSN: 0163-3864
  1. Abstract:

    A high-throughput cell-based reporter assay designed to identify small-molecule stabilizers of the tumor suppressor Pdcd4 was used to screer. extracts in the NCI Natural Products Repository. Bioassay-guided fractionation of an extract from a Papua New Guinea collection of the tropical tree Cryptocarya sp. provided a series of new 5,6-dihydro-alpha-pyrone-containing 1,3-polyols (1-8), named cryptocaryols A-H. Their structures were assigned from a combination of NMR, MS, and CD studies in conjunction with NMR database comparisons. Compounds 1-8 were found to rescue Pdcd4 from TPA-induced degradation with EC(50) concentrations that ranged from 1.3 to 4.9 mu M.

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External Sources

  1. DOI: 10.1021/np100918z
  2. WOS: 000291127900015

Library Notes

  1. Fiscal Year: FY2010-2011
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