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Synthesis and structure-activity relationship of botryllamides that block the ABCG2 multidrug transporter

  1. Author:
    Takada, K.
    Imamura, N.
    Gustafson, K. R.
    Henrich, C. J.

  2. Author Address

    [Takada, Kentaro; Imamura, Nobutaka] Ritsumeikan Univ, Lab Microbial Chem, Coll Pharmaceut Sci, Shiga 5258577, Japan. [Gustafson, Kirk R.; Henrich, Curtis J.] NCI, Mol Targets Lab, Ctr Canc Res, Frederick, MD 21702 USA. [Henrich, Curtis J.] SAIC Frederick Inc, Basic Res Program, Frederick, MD 21702 USA.;Takada, K, Ritsumeikan Univ, Lab Microbial Chem, Coll Pharmaceut Sci, 1-1-1 Noji Higashi, Shiga 5258577, Japan.;takada@ph.ritsumei.ac.jp
    1. Year: 2010
    2. Date: Feb
  2. Journal: Bioorganic & Medicinal Chemistry Letters
    1. 20
    2. 4
    3. Pages: 1330-1333
  4. Type of Article: Article
  5. ISSN: 0960-894X
  1. Abstract:

    In previous work, botryllamides discovered from the marine ascidian Botryllus tyreus were characterized as selective inhibitors of the ABCG2 multidrug transporter. However, the structural basis for this activity could not be established. In this study, botryllamide F, the core botryllamide structure, and botryllamide G, the most potent botryllamide ABCG2 inhibitor, were synthesized along with a series of structural variants for evaluation of structure - activity relationships. The biological activity of synthetic botryllamide analogs implied that the 2-methoxy-p-coumaric acid portion, and the degree of double bond conjugation within this group, were critical for inhibition of ABCG2. However, variations in the substituents on the two aryl groups did not appear to significantly impact the potency or degree of inhibition. (C) 2010 Elsevier Ltd. All rights reserved.

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External Sources

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  2. DOI: 10.1016/j.bmcl.2010.01.016
  3. View record in Web of Science®
  4. WOS: 000274285600002

Library Notes

  1. Fiscal Year: FY2009-2010
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