Abstract
A novel series of dual EGFR and HER2 inhibitors based on the pyrrolo[2,1-f][1,2,4]triazine nucleus is described. A general route toward their synthesis, which enables functionalization at multiple sites, has been developed. Biological evaluation in enzymatic and cell-based assays has identified a series of C-6 carbamates with potent biochemical and cellular activities.
MeSH terms
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Binding Sites
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Carbamates / chemical synthesis
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Carbamates / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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ErbB Receptors / antagonists & inhibitors*
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Humans
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Models, Molecular
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Receptor Protein-Tyrosine Kinases / antagonists & inhibitors*
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Receptor, ErbB-2 / antagonists & inhibitors*
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Structure-Activity Relationship
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Triazines / chemical synthesis
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Triazines / pharmacology
Substances
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Carbamates
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Triazines
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ErbB Receptors
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Receptor Protein-Tyrosine Kinases
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Receptor, ErbB-2