title: 2-Guanidinoquinazolines as new inhibitors of the STAT3 pathway.
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.
authors.affiliation: University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA. Electronic address: mgl12@pitt.edu.
authors.forename: Matthew G
authors.initials: MG
authors.lastname: LaPorte
authors.affiliation: University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA.
authors.forename: Dimas José
authors.initials: DJ
authors.lastname: da Paz Lima
authors.affiliation: University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA.
authors.forename: Feng
authors.initials: F
authors.lastname: Zhang
authors.affiliation: Department of Otolaryngology, University of Pittsburgh, Pittsburgh, PA 15260, USA.
authors.forename: Malabika
authors.initials: M
authors.lastname: Sen
authors.affiliation: 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.
authors.forename: Jennifer R
authors.initials: JR
authors.lastname: Grandis
authors.affiliation: Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA.
authors.forename: Daniel
authors.initials: D
authors.lastname: Camarco
authors.affiliation: Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA.
authors.forename: Yun
authors.initials: Y
authors.lastname: Hua
authors.affiliation: University of Pittsburgh Cancer Institute, Pittsburgh, PA 15260, USA; Department of Pharmaceutical Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA.
authors.forename: Paul A
authors.initials: PA
authors.lastname: Johnston
authors.affiliation: Department of Pharmacology, University of Virginia, Charlottesville, VA 22908, USA.
authors.forename: John S
authors.initials: JS
authors.lastname: Lazo
authors.affiliation: University of Pittsburgh Chemical Diversity Center, University of Pittsburgh, Pittsburgh, PA 15260, USA.
authors.forename: Lynn O
authors.initials: LO
authors.lastname: Resnick
authors.affiliation: 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.
authors.forename: Peter
authors.initials: P
authors.lastname: Wipf
authors.affiliation: 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: huryn@pitt.edu.
authors.forename: Donna M
authors.initials: DM
authors.lastname: Huryn
mesh_terms: D017209:Apoptosis / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D019791:Guanidine / Q000737:chemistry*; D006801:Humans; D011485:Protein Binding; D011799:Quinazolines / Q000737:chemistry* / Q000378:metabolism / Q000633:toxicity; D050796:STAT3 Transcription Factor / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D011799:Quinazolines; D050796:STAT3 Transcription Factor; D019791:Guanidine
keywords: Cancer cell line screening; Guanidinoquinazolines; STAT3 pathway; Skraup synthesis; Structure–activity relationships