Abstract
The microwave-assisted synthesis of a family of 2,8-substituted thiazoloquinazolinones is described. The preliminary evaluation of the antiproliferative activity and the capacity of these molecules to inhibit CDKs and GSK-3 are reported. A lead compound was identified, constituting a scaffold from which more potent inhibitors could be designed.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Cell Line, Tumor
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Cell Proliferation / drug effects
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Cyclin-Dependent Kinases / antagonists & inhibitors*
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Drug Evaluation, Preclinical
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Enzyme Inhibitors / chemical synthesis*
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Enzyme Inhibitors / pharmacology*
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Enzyme Inhibitors / radiation effects
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Glycogen Synthase Kinase 3 / antagonists & inhibitors*
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Humans
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Microwaves
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Molecular Structure
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Quinazolines / chemical synthesis*
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Quinazolines / pharmacology*
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Quinazolines / radiation effects
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Quinazolines
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Cyclin-Dependent Kinases
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Glycogen Synthase Kinase 3