Abstract
Continuous efforts in microwave-assisted synthesis and the structure-activity relationships' (SARs) studies of novel modified 9-oxo-thiazolo[5,4-f]quinazoline-2-carbonitriles, allowed identification of new amidine and imidate derivatives as potent and dual CDK1/GSK-3 inhibitors. Combination of lead optimization and molecular modeling studies allowed identification of a dual CDK1/GSK-3 inhibitor (compound 13d) with submicromolar values.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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CDC2 Protein Kinase / antagonists & inhibitors*
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Enzyme Inhibitors / pharmacology*
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Glycogen Synthase Kinase 3 / antagonists & inhibitors*
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Magnetic Resonance Spectroscopy
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Models, Molecular*
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Nitriles / chemical synthesis*
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Nitriles / pharmacology*
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Quinazolines / chemical synthesis*
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Quinazolines / pharmacology*
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Spectrophotometry, Infrared
Substances
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9-oxo-thiazolo(5,4-f)quinazoline-2-carbonitrile
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Enzyme Inhibitors
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Nitriles
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Quinazolines
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CDC2 Protein Kinase
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Glycogen Synthase Kinase 3