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Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer

  1. Author:
    Choudhary, Shruti
    Doshi, Arpit
    Luckett-Chastain, Lerin
    Ihnat, Michael
    Hamel,Ernest
    Mooberry, Susan L.
    Gangjee, Aleem

  2. Author Address

    Duquesne Univ, Grad Sch Pharmaceut Sci, Div Med Chem, 600 Forbes Ave, Pittsburgh, PA 15282 USA.Univ Oklahoma, Coll Pharm, Hlth Sci Ctr, 1110 North Stonewall, Oklahoma City, OK 73117 USA.NCI, Mol Pharmacol Branch, Dev Therapeut Program,NIH, Div Canc Treatment & Diag,Frederick Natl Lab Canc, Frederick, MD 21702 USA.Univ Texas Hlth Sci Ctr, Mays Canc Ctr, Dept Pharmacol, 7703 Floyd Curl Dr, San Antonio, TX 78229 USA.Scripps Res Inst, Jupiter, FL 33458 USA.
    1. Year: 2021
    2. Date: Apr 1
    3. Epub Date: 2021 Feb 12
  2. Journal: Bioogranic & Medicinal Chemistry
  3. Pergamon-Elsevier Science Ltd.
    1. 35
  5. Type of Article: Article
  6. Article Number: ARTN 116061
  7. ISSN: 0968-0896
  1. Abstract:

    The efficacy of quinazoline-based antiglioma agents has been attributed to their effects on microtubule dynamics.1,2 The design, synthesis and biological evaluation of quinazolines as potent inhibitors of multiple intracellular targets, including microtubules and multiple RTKs, is described. In addition to the known ability of quinazolines 1 and 2 to cause microtubule depolymerization, they were found to be low nanomolar inhibitors of EGFR, VEGFR-2 and PDGFR-?. Low nanomolar inhibition of EGFR was observed for 1?3 and 9?10. Compounds 1 and 4 inhibited VEGFR-2 kinase with activity better than or equal to that of sunitinib. In addition, compounds 1 and 2 had similar potency to sunitinib in the CAM angiogenesis assay. Multitarget activities of compounds in the present study demonstrates that the quinazolines can affect multiple pathways and could lead to these agents having antitumor potential caused by their activity against multiple targets.

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External Sources

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  2. DOI: 10.1016/j.bmc.2021.116061
  3. PMID: 33647840
  4. PMCID: PMC7995636
  5. View record in Web of Science®
  6. WOS: 000632527600003

Library Notes

  1. Fiscal Year: FY2020-2021
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