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

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

Research output: Contribution to journalArticlepeer-review


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-β. 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.

Original languageEnglish (US)
Article number116061
JournalBioorganic and Medicinal Chemistry
StatePublished - Apr 1 2021
Externally publishedYes


  • Angiogenesis
  • Microtubule targeting agents
  • Multi-target inhibitors
  • Quinazolines
  • Receptor tyrosine kinase

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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