2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway

Bioorg Med Chem Lett. 2014 Nov 1;24(21):5081-5. doi: 10.1016/j.bmcl.2014.09.001. Epub 2014 Sep 15.

Abstract

Synthesis and SAR investigation of 2-guanidinoquinazolines, initially identified in a high content screen for selective STAT3 pathway inhibitors, led to a more potent analog (11c) that demonstrated improved anti-proliferative activity against a panel of HNSCC cell lines.

Keywords: Cancer cell line screening; Guanidinoquinazolines; STAT3 pathway; Skraup synthesis; Structure–activity relationships.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Apoptosis / drug effects
  • Cell Line, Tumor
  • Cell Proliferation / drug effects
  • Guanidine / chemistry*
  • Humans
  • Protein Binding
  • Quinazolines / chemistry*
  • Quinazolines / metabolism
  • Quinazolines / toxicity
  • STAT3 Transcription Factor / antagonists & inhibitors*
  • STAT3 Transcription Factor / metabolism
  • Structure-Activity Relationship

Substances

  • Quinazolines
  • STAT3 Transcription Factor
  • Guanidine