Abstract
The tyrosine kinase activity of the epidermal growth factor receptor (EGFR) is widely involved in signaling pathways and often deregulated in cancer. Its role in the development of prostate cancer is well established, and therapeutic strategies such as blockade of the intracellular tyrosine kinase domain with small-molecule tyrosine kinase inhibitors have been proposed. Herein we describe the synthesis and in vitro pharmacological properties of C6- and C7-substituted 4-anilinoquinazolines, analogues of Iressa and powerful proapoptotic inducers in hormone-independent prostate cancer PC3 cell lines.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / pharmacology*
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Apoptosis / drug effects*
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Apoptosis / physiology
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Cell Line, Tumor
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ErbB Receptors / antagonists & inhibitors*
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ErbB Receptors / metabolism
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Gefitinib
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Humans
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Male
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Prostatic Neoplasms / drug therapy*
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Prostatic Neoplasms / pathology
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / pharmacology*
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Protein-Tyrosine Kinases / antagonists & inhibitors*
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Quinazolines / chemical synthesis
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Quinazolines / pharmacology*
Substances
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Antineoplastic Agents
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Protein Kinase Inhibitors
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Quinazolines
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ErbB Receptors
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Protein-Tyrosine Kinases
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Gefitinib