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Methanesulfonamido-cyclohexylamine derivatives of 2,4-diaminopyrimidine as potent ALK inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jul 01; Vol. 21 (13), pp. 3877-80. Date of Electronic Publication: 2011 May 18. - Publication Year :
- 2011
-
Abstract
- The incorporation of R,R-1,2-diaminocyclohexane at C4 in a series of 2,4-diaminopyrimidines led to a number of ALK inhibitors in which optimized activity was achieved by conversion of the 2-amino group into a methanesulfonamide. Tumor growth inhibition was observed when an orally bioavailable analog was evaluated in a Karpas-299 tumor xenograft mouse model.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Administration, Oral
Anaplastic Lymphoma Kinase
Animals
Antineoplastic Agents administration & dosage
Antineoplastic Agents pharmacology
Cyclohexylamines administration & dosage
Cyclohexylamines pharmacology
Enzyme Activation drug effects
Enzyme Inhibitors administration & dosage
Enzyme Inhibitors chemical synthesis
Enzyme Inhibitors pharmacology
Infusion Pumps
Inhibitory Concentration 50
Mice
Molecular Structure
Neoplasms drug therapy
Pyrimidines administration & dosage
Pyrimidines pharmacology
Rats
Rats, Sprague-Dawley
Xenograft Model Antitumor Assays
Antineoplastic Agents chemical synthesis
Cyclohexylamines chemical synthesis
Pyrimidines chemical synthesis
Receptor Protein-Tyrosine Kinases antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 13
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21632243
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.05.040