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Design and synthesis of novel 3-sulfonylpyrazol-4-amino pyrimidines as potent anaplastic lymphoma kinase (ALK) inhibitors.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2016 Apr 15; Vol. 26 (8), pp. 1910-8. Date of Electronic Publication: 2016 Mar 07. - Publication Year :
- 2016
-
Abstract
- Anaplastic lymphoma kinase (ALK) is a highly attractive therapeutic target for the treatment of some non-small cell lung cancer patients. This Letter describes the further SAR exploration on the novel 3-sulfonylpyrazol-4-amino pyrimidine scaffold. This work identified a compound 53 with very good in vitro/in vivo efficacies, good DMPK properties together with better hERG tolerability and it is currently being profiled for the evaluation as a potential pre-clinical candidate.<br /> (Copyright © 2016 Elsevier Ltd. All rights reserved.)
- Subjects :
- Anaplastic Lymphoma Kinase
Animals
Antineoplastic Agents chemical synthesis
Antineoplastic Agents chemistry
Cell Line, Tumor
Cell Proliferation drug effects
Dogs
Dose-Response Relationship, Drug
Drug Screening Assays, Antitumor
Humans
Mice
Models, Molecular
Molecular Structure
Neoplasms, Experimental drug therapy
Neoplasms, Experimental pathology
Protein Kinase Inhibitors chemical synthesis
Protein Kinase Inhibitors chemistry
Pyrazoles chemistry
Pyrimidines chemistry
Rats
Receptor Protein-Tyrosine Kinases metabolism
Structure-Activity Relationship
Antineoplastic Agents pharmacology
Drug Design
Protein Kinase Inhibitors pharmacology
Pyrazoles chemical synthesis
Pyrazoles pharmacology
Pyrimidines chemical synthesis
Pyrimidines pharmacology
Receptor Protein-Tyrosine Kinases antagonists & inhibitors
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 26
- Issue :
- 8
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 26979157
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.03.017