Skip NavigationSkip to Content
Return Return to Search Results

A boronic acid chalcone analog of combretastatin A-4 as a potent anti-proliferation agent

  1. Author:
    Kong, Y. L.
    Wang, K.
    Edler, M. C.
    Hamel, E.
    Mooberry, S. L.
    Paige, M. A.
    Brown, M. L.

  2. Author Address

    [Kong, Yali; Wang, Kan; Paige, Mikell A.; Brown, Milton L.] Georgetown Univ, Med Ctr, Dept Oncol, Drug Discovery Program, Washington, DC 20057 USA. [Wang, Kan; Edler, Michael C.] NCI, Toxicol & Pharmacol Branch, Dev Therapeut Program, Div Canc Treatment & Diag,NIH, Frederick, MD 21702 USA. [Mooberry, Susan L.] SW Fdn Biomed Res, Dept Physiol & Med, San Antonio, TX 78245 USA.;Brown, ML, Georgetown Univ, Med Ctr, Dept Oncol, Drug Discovery Program, 3970 Reservoir Rd, Washington, DC 20057 USA.;mb544@georgetown.edu
    1. Year: 2010
    2. Date: Jan
  2. Journal: Bioorganic & Medicinal Chemistry
    1. 18
    2. 2
    3. Pages: 971-977
  4. Type of Article: Article
  5. ISSN: 0968-0896
  1. Abstract:

    Chalcones represent a class of natural products that inhibits tubulin assembly. In this study we designed and synthesized boronic acid analogs of chalcones in an effort to compare biological activities with combretastatin A-4, a potent inhibitor of tubulin polymerization. Systematic evaluation of the positional effects of the carbonyl moiety towards inhibition of tubulin polymerization, cancer cell proliferation and angiogenesis revealed that placement of the carbonyl adjacent to the trimethoxybenzene A-ring resulted in more active compounds than when the carbonyl group was placed adjacent to the C-ring. Our study identified a boronic acid chalcone with inhibition towards 16 human cancer cell lines in the 10-200 nM range, and another three cell lines with GI(50)-values below 10 nM. Furthermore, this drug has significant anti-angiogenesis effects demonstrated by HUVEC tube formation and aortic ring assay. (C) 2009 Elsevier Ltd. All rights reserved.

    See More

  1. Keywords:

External Sources

  1. View Full Text
  2. DOI: 10.1016/j.bmc.2009.11.003
  3. View record in Web of Science®
  4. WOS: 000273613500052

Library Notes

  1. Fiscal Year: FY2009-2010
NCI at Frederick

You are leaving a government website.

This external link provides additional information that is consistent with the intended purpose of this site. The government cannot attest to the accuracy of a non-federal site.

Linking to a non-federal site does not constitute an endorsement by this institution or any of its employees of the sponsors or the information and products presented on the site. You will be subject to the destination site's privacy policy when you follow the link.

ContinueCancel