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Discovery of 2,4-bis-arylamino-1,3-pyrimidines as insulin-like growth factor-1 receptor (IGF-1R) inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Apr 15; Vol. 21 (8), pp. 2394-9. Date of Electronic Publication: 2011 Feb 23. - Publication Year :
- 2011
-
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.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Binding Sites
Crystallography, X-Ray
Drug Evaluation, Preclinical
Humans
Mice
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors pharmacokinetics
Pyrimidines chemical synthesis
Pyrimidines pharmacokinetics
Quinolines chemistry
Quinolines pharmacokinetics
Receptor, IGF Type 1 metabolism
Structure-Activity Relationship
Xenograft Model Antitumor Assays
Protein Kinase Inhibitors chemistry
Pyrimidines chemistry
Quinolines chemical synthesis
Receptor, IGF Type 1 antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21414779
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.02.075