2. Academic Validation
  3. 2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway

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.
Matthew G LaPorte 1,  Dimas José da Paz Lima 2,  Feng Zhang 2,  Malabika Sen 3,  Jennifer R Grandis 4,  Daniel Camarco 5,  Yun Hua 5,  Paul A Johnston 6,  John S Lazo 7,  Lynn O Resnick 2,  Peter Wipf 8,  Donna M Huryn 9
Affiliations

Affiliations

  • 1 University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA. Electronic address: [email protected].
  • 2 University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA.
  • 3 Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA.
  • 4 Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA; University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA; Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, PA 15260, USA.
  • 5 Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA.
  • 6 University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA; Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA.
  • 7 Department of Pharmacology, University of Virginia, Charlottesville, VA 22908, USA.
  • 8 University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA; University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA; Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA.
  • 9 University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA; Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA. Electronic address: [email protected].
PMID: 25288188 DOI: 10.1016/j.bmcl.2014.09.001
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.

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