Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3
- PMID: 21106455
- DOI: 10.1016/j.bmcl.2010.10.026
Diamino-1,2,4-triazole derivatives are selective inhibitors of TYK2 and JAK1 over JAK2 and JAK3
Abstract
Tyrosine kinase 2 (TYK2) is required for signaling of interleukin-23 (IL-23), which plays a key role in rheumatoid arthritis. Presented is the design and synthesis of 1,2,4-triazoles, and the evaluation of their inhibitory activity against the Janus associated kinases TYK2 and JAKs 1-3.
Copyright © 2010 Elsevier Ltd. All rights reserved.
Similar articles
-
The discovery of 2,5-isomers of triazole-pyrrolopyrimidine as selective Janus kinase 2 (JAK2) inhibitors versus JAK1 and JAK3.Bioorg Med Chem. 2016 Nov 1;24(21):5036-5046. doi: 10.1016/j.bmc.2016.08.008. Epub 2016 Aug 6. Bioorg Med Chem. 2016. PMID: 27555284
-
Discovery of potent and efficacious pyrrolopyridazines as dual JAK1/3 inhibitors.Bioorg Med Chem Lett. 2017 Jul 15;27(14):3101-3106. doi: 10.1016/j.bmcl.2017.05.043. Epub 2017 May 15. Bioorg Med Chem Lett. 2017. PMID: 28539220
-
9H-Carbazole-1-carboxamides as potent and selective JAK2 inhibitors.Bioorg Med Chem Lett. 2015 Jul 15;25(14):2809-12. doi: 10.1016/j.bmcl.2015.04.101. Epub 2015 May 11. Bioorg Med Chem Lett. 2015. PMID: 25987372
-
Selective JAK1 inhibitor and selective Tyk2 inhibitor patents.Expert Opin Ther Pat. 2012 Oct;22(10):1233-49. doi: 10.1517/13543776.2012.723693. Epub 2012 Sep 13. Expert Opin Ther Pat. 2012. PMID: 22971156 Review.
-
Inhibitors of JAK2 and JAK3: an update on the patent literature 2010 - 2012.Expert Opin Ther Pat. 2013 Apr;23(4):449-501. doi: 10.1517/13543776.2013.765862. Epub 2013 Feb 1. Expert Opin Ther Pat. 2013. PMID: 23367873 Review.
Cited by
-
Molecular dynamics and integrated pharmacophore-based identification of dual [Formula: see text] inhibitors.Mol Divers. 2018 Feb;22(1):95-112. doi: 10.1007/s11030-017-9794-z. Epub 2017 Nov 14. Mol Divers. 2018. PMID: 29138965
-
A Novel Strategy for Regulating mRNA's Degradation via Interfering the AUF1's Binding to mRNA.Molecules. 2022 May 16;27(10):3182. doi: 10.3390/molecules27103182. Molecules. 2022. PMID: 35630659 Free PMC article.
-
Targeted kinase selectivity from kinase profiling data.ACS Med Chem Lett. 2012 Mar 14;3(5):383-6. doi: 10.1021/ml300012r. eCollection 2012 May 10. ACS Med Chem Lett. 2012. PMID: 24900482 Free PMC article.
-
Analyzing Resistance to Design Selective Chemical Inhibitors for AAA Proteins.Cell Chem Biol. 2019 Sep 19;26(9):1263-1273.e5. doi: 10.1016/j.chembiol.2019.06.001. Epub 2019 Jun 27. Cell Chem Biol. 2019. PMID: 31257183 Free PMC article.
-
Dual inhibitors of Janus kinase 2 and 3 (JAK2/3): designing by pharmacophore- and docking-based virtual screening approach.Mol Divers. 2014 May;18(2):253-67. doi: 10.1007/s11030-013-9497-z. Epub 2014 Jan 11. Mol Divers. 2014. PMID: 24415188
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Other Literature Sources
Chemical Information
Molecular Biology Databases
Research Materials
Miscellaneous