Abstract
A series of C-6 or C-3' alkynyl-substituted 4-anilinoquinazoline derivatives was prepared straightforwardly by a Sonogashira reaction of the corresponding bromo-substituted 4-anilinoquinazolines. Bioactive assay of these compounds for in vitro EGFR kinase inhibition demonstrated that the novel 6-hydroxypropynyl-4-anilinoquinazoline 5e was a very potent EGFR kinase inhibitor with an IC(50) of 14 nM.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Aniline Compounds / chemical synthesis*
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Aniline Compounds / chemistry
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Aniline Compounds / pharmacology*
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Antineoplastic Agents / chemical synthesis*
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Antineoplastic Agents / chemistry
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Antineoplastic Agents / pharmacology*
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Computer Simulation
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Drug Screening Assays, Antitumor
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ErbB Receptors / antagonists & inhibitors*
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Inhibitory Concentration 50
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Models, Molecular
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Molecular Structure
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Quinazolines / chemical synthesis*
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Quinazolines / chemistry
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Quinazolines / pharmacology*
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Structure-Activity Relationship
Substances
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6-hydroxypropynyl-4-anilinoquinazoline
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Aniline Compounds
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Antineoplastic Agents
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Quinazolines
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ErbB Receptors