Abstract
2,7-Diamino-thiazolo[4,5-d]pyrimidine analogues were synthesized as novel epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors. Representative compounds showed potent and selective EGFR inhibitory activities and inhibited in vitro cellular proliferation in EGFR-overexpressing human tumor cells. The synthesis and preliminary biological, physical, and pharmacokinetic evaluation of these thiazolopyrimidine compounds are reported.
MeSH terms
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Drug Screening Assays, Antitumor / methods
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ErbB Receptors / antagonists & inhibitors*
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Humans
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Protein Kinase Inhibitors / analogs & derivatives*
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / pharmacology
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Pyrimidines / chemical synthesis*
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Pyrimidines / pharmacology
Substances
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Antineoplastic Agents
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Protein Kinase Inhibitors
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Pyrimidines
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ErbB Receptors