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

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-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 demonst

SUBMITTER: Choudhary S 

PROVIDER: S-EPMC7995636 | biostudies-literature | 2021 Apr

REPOSITORIES: biostudies-literature