Novel conjugates of endoperoxide and 4-anilinoquinazoline as potential anticancer agents

Bioorg Med Chem Lett. 2017 Mar 15;27(6):1341-1345. doi: 10.1016/j.bmcl.2017.02.023. Epub 2017 Feb 13.

Abstract

In the present study, endoperoxide and 4-anilinoqnazoline were conjugated to obtain a series of compounds. These conjugates exhibited high antiproliferative potency against a number of cancer cell lines, including the epidermal growth factor receptor (EGFR) L858R/T790M mutant cell. Compound 5 was selected as a representative for mechanistic study. Further experiments revealed the conjugate's reactive oxygen species (ROS) generating ability, apoptosis inducing activity and involvement in EGFR downstream signaling pathways.

Keywords: 4-Anilinoquinazoline; Anti-cancer agents; Conjugates; EGFR-TKI; Endoperoxide.

MeSH terms

  • Antineoplastic Agents / chemistry
  • Antineoplastic Agents / pharmacology*
  • Cell Line, Tumor
  • ErbB Receptors / antagonists & inhibitors
  • Humans
  • Inhibitory Concentration 50
  • Peroxides / chemistry*
  • Quinazolines / chemistry*

Substances

  • Antineoplastic Agents
  • Peroxides
  • Quinazolines
  • ErbB Receptors