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Discovery of novel tetracyclic compounds as anaplastic lymphoma kinase inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jun 15; Vol. 21 (12), pp. 3788-93. Date of Electronic Publication: 2011 Apr 22. - Publication Year :
- 2011
-
Abstract
- Anaplastic lymphoma kinase (ALK) receptor tyrosine kinase is considered a promising therapeutic target for human cancers. We identified novel tetracyclic derivatives as potent ALK inhibitors. Among them, compound 27 showed strong cytotoxicity against KARPAS-299 with an IC(50) value of 21 nM and significant antitumor efficacy in ALK fusion-positive blood and solid cancer xenograft models in mice without body weight loss.<br /> (Copyright © 2011 Elsevier Ltd. All rights reserved.)
- Subjects :
- Anaplastic Lymphoma Kinase
Animals
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Disease Models, Animal
Enzyme Activation drug effects
Humans
Inhibitory Concentration 50
Mice
Molecular Structure
Tetracyclines chemistry
Tetracyclines pharmacology
Antineoplastic Agents chemical synthesis
Drug Discovery
Receptor Protein-Tyrosine Kinases antagonists & inhibitors
Tetracyclines chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21561771
- Full Text :
- https://doi.org/10.1016/j.bmcl.2011.04.020