Abstract
A series of new 2-(2-aminopyrimidin-4-yl)phenol derivatives were synthesized as potential antitumor compounds. Substitution with pyrrolidine-3,4-diol at the 4-position of phenol provided potent inhibitory activity against CDK1 and CDK2. X-ray crystal structural studies were performed to account for the effect of the substituent on both the enzymatic and cell growth inhibitory activities.
Copyright © 2011 Elsevier Ltd. All rights reserved.
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 / chemistry*
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Antineoplastic Agents / toxicity
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Binding Sites
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CDC2 Protein Kinase / antagonists & inhibitors*
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CDC2 Protein Kinase / metabolism
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Cell Line, Tumor
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Computer Simulation
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Cyclin-Dependent Kinase 2 / antagonists & inhibitors*
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Cyclin-Dependent Kinase 2 / metabolism
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Drug Evaluation, Preclinical
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Drug Screening Assays, Antitumor
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Humans
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Protein Kinase Inhibitors / chemical synthesis
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Protein Kinase Inhibitors / chemistry*
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Protein Kinase Inhibitors / toxicity
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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / toxicity
Substances
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Antineoplastic Agents
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Protein Kinase Inhibitors
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Pyrimidines
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2-aminopyrimidine
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CDC2 Protein Kinase
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Cyclin-Dependent Kinase 2