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Inhibition of ABCG2-mediated drug efflux by naphthopyrones from marine crinoids

  1. Author:
    Bokesch, H. R.
    Cartner, L. K.
    Fuller, R. W.
    Wilson, J. A.
    Henrich, C. J.
    Kelley, J. A.
    Gustafson, K. R.
    McMahon, J. B.
    McKee, T. C.

  2. Author Address

    [Bokesch, Heidi R.; Cartner, Laura K.; Fuller, Richard W.; Wilson, Jennifer A.; Henrich, Curtis J.; Gustafson, Kirk R.; McMahon, James B.; McKee, Tawnya C.] NCI, Mol Targets Lab, Frederick, MD 21702 USA. [Bokesch, Heidi R.; Cartner, Laura K.; Henrich, Curtis J.] NCI, SAIC Frederick Inc, Frederick, MD 21702 USA. [Kelley, James A.] NCI, Biol Chem Lab, Frederick, MD 21702 USA.;McKee, TC, NCI, Mol Targets Lab, Frederick, MD 21702 USA.;mckeeta@mail.nih.gov
    1. Year: 2010
    2. Date: Jul
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 20
    2. 13
    3. Pages: 3848-3850
  4. Type of Article: Article
  5. ISSN: 0960-894X
  1. Abstract:

    Five new naphthopyrones (1-5) along with the known compounds TMC-256A1, 5,8-dihydroxy-6-methoxy-2-propyl-4H-naphtho[2,3-b]pyran-4-one, TMC-256C1, comaparvin, 6-methoxycomaparvin, and 6-methoxycomaparvin 5-methyl ether (6-11) were isolated from crinoids of the family Comasteridae. All compounds were tested for their ability to inhibit the multidrug transporter ABCG2, which plays a role in drug resistance. Six of the seven angular naphthopyrones showed moderate activity with <60% inhibition of ABCG2-mediated transport as compared to the positive control fumitremorgin C. None of the linear naphthopyrones inhibited ABCG2-mediated efflux. Published by Elsevier Ltd.

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External Sources

  1. View Full Text
  2. DOI: 10.1016/j.bmcl.2010.05.057
  3. View record in Web of Science®
  4. WOS: 000278644700002

Library Notes

  1. Fiscal Year: FY2009-2010
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