Abstract
The structure-activity and structure-property relationships of anilinoquinazoline inhibitors of EGFR were investigated. Strategies to lower volume of distribution and shorten half-life through structure and pKa modulation are discussed.
MeSH terms
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Animals
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Antineoplastic Agents / chemical synthesis
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacokinetics
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Antineoplastic Agents / pharmacology
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Cell Line, Tumor
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Chemical Phenomena
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Chemistry, Physical
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ErbB Receptors / antagonists & inhibitors*
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ErbB Receptors / metabolism
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Fluorine / chemistry
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Gefitinib
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Humans
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Inhibitory Concentration 50
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Mice
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Molecular Structure
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Neoplasms / drug therapy
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Neoplasms / pathology
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Protein Kinase Inhibitors / chemical synthesis*
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Protein Kinase Inhibitors / chemistry
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Protein Kinase Inhibitors / pharmacokinetics*
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Protein Kinase Inhibitors / pharmacology
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Quinazolines / chemistry
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Rats
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Structure-Activity Relationship
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Thiazoles / chemistry
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Xenograft Model Antitumor Assays
Substances
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Antineoplastic Agents
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Protein Kinase Inhibitors
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Quinazolines
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Thiazoles
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Fluorine
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2-anilino-5-thiazolinone
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ErbB Receptors
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Gefitinib