Abstract
The insulin-like growth factor-1 receptor (IGF-1R) plays an important role in the regulation of cell growth and differentiation, and in protection from apoptosis. IGF-1R has been shown to be an appealing target for the treatment of human cancer. Herein, we report the synthesis, structure-activity relationships (SAR), X-ray cocrystal structure and in vivo tumor study results for a series of 2,4-bis-arylamino-1,3-pyrimidines.
Copyright © 2011 Elsevier Ltd. All rights reserved.
MeSH terms
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Animals
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Binding Sites
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Crystallography, X-Ray
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Drug Evaluation, Preclinical
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Humans
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Mice
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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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Pyrimidines / chemical synthesis
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Pyrimidines / chemistry*
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Pyrimidines / pharmacokinetics
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Quinolines / chemical synthesis*
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Quinolines / chemistry
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Quinolines / pharmacokinetics
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Receptor, IGF Type 1 / antagonists & inhibitors*
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Receptor, IGF Type 1 / metabolism
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Structure-Activity Relationship
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Xenograft Model Antitumor Assays
Substances
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Protein Kinase Inhibitors
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Pyrimidines
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Quinolines
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Receptor, IGF Type 1