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Design, synthesis and biological evaluation of hybrid nitroxide-based non-steroidal anti-inflammatory drugs

  1. Author:
    Thomas, Komba
    Moody, Terry
    Jensen, Robert
    Tong, Jason
    Rayner, Cassie L
    Barnett, Nigel L
    Fairfull-Smith, Kathryn E
    Ridnour, Lisa
    Wink, David
    Bottle, Steven E

  2. Author Address

    School of Chemistry, Physics and Mechanical Engineering, Queensland University of Technology, (QUT) GPO Box 2434, Brisbane, QLD 4001, Australia., Center for Cancer Research, National Cancer Institute, Cancer and Inflammation Program, Frederick, MD 21702-1201, USA., Queensland Eye Institute, South Brisbane, Queensland, Australia., Queensland Eye Institute, South Brisbane, Queensland, Australia; The University of Queensland, UQ Centre for Clinical Research, Herston, Queensland, Australia., School of Chemistry, Physics and Mechanical Engineering, Queensland University of Technology, (QUT) GPO Box 2434, Brisbane, QLD 4001, Australia. Electronic address: s.bottle@qut.edu.au.,
    1. Year: 2018
    2. Date: Mar 10
    3. Epub Date: 2018 01 31
  2. Journal: European journal of medicinal chemistry
    1. 147
    2. Pages: 34-47
  4. Type of Article: Article
  5. ISSN: 0223-5234
  1. Abstract:

    Dual-acting hybrid anti-oxidant/anti-inflammatory agents were developed employing the principle of pharmacophore hybridization. Hybrid agents were synthesized by combining stable anti-oxidant nitroxides with conventional non-steroidal anti-inflammatory drugs (NSAIDs). Several of the hybrid nitroxide-NSAID conjugates displayed promising anti-oxidant and anti-inflammatory effects on two Non-Small Cell Lung Cancer (NSCLC) cells (A549 and NCI-H1299) and in ameliorating oxidative stress induced in 661?W retinal cells. One ester-linked nitroxide-aspirin analogue (27) delivered better anti-inflammatory effects (cyclooxygenase inhibition) than the parent compound (aspirin), and also showed similar reactive oxygen scavenging activity to the anti-oxidant, Tempol. In addition, a nitroxide linked to the anti-inflammatory drug indomethacin (39) significantly ameliorated the effects of oxidative stress on 661?W retinal neurons at efficacies greater or equal to the anti-oxidant Lutein. Other examples of the hybrid conjugates displayed promising anti-cancer activity, as demonstrated by their inhibitory effects on the proliferation of A549 NSCLC cells. Copyright © 2018. Published by Elsevier Masson SAS.

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External Sources

  1. View Full Text
  2. DOI: 10.1016/j.ejmech.2018.01.077
  3. PMID: 29421569
  4. View record in Web of Science®
  5. WOS: 000427217100004
  6. PII : S0223-5234(18)30096-5

Library Notes

  1. Fiscal Year: FY2017-2018
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