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.
Copyright © 2014 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Apoptosis / drug effects
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Guanidine / chemistry*
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Humans
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Protein Binding
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Quinazolines / chemistry*
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Quinazolines / metabolism
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Quinazolines / toxicity
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STAT3 Transcription Factor / antagonists & inhibitors*
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STAT3 Transcription Factor / metabolism
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Structure-Activity Relationship
Substances
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Quinazolines
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STAT3 Transcription Factor
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Guanidine