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Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2.
- Source :
-
European journal of medicinal chemistry [Eur J Med Chem] 2011 Mar; Vol. 46 (3), pp. 870-6. Date of Electronic Publication: 2011 Jan 09. - Publication Year :
- 2011
-
Abstract
- A novel series of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids has been synthesized and tested in vitro towards human protein kinase CK2. It was revealed that the most active compounds inhibiting CK2 are 3-{[5-(4-methylphenyl)thieno[2,3-d]pyrimidin-4-yl]thio}propanoic acid and 3-{[5-(4-ethoxyphenyl)thieno[2,3-d]pyrimidin-4-yl]thio}propanoic acid (IC(50) values are 0.1 μM and 0.125 μM, respectively). Structure-activity relationships of 28 tested thienopyrimidine derivatives have been studied and binding mode of this chemical class has been predicted. Evaluation of the inhibitors on seven protein kinases revealed considerable selectivity towards CK2.<br /> (Copyright © 2011 Elsevier Masson SAS. All rights reserved.)
- Subjects :
- Carboxylic Acids chemical synthesis
Carboxylic Acids chemistry
Carboxylic Acids pharmacology
Humans
Models, Molecular
Protein Kinase Inhibitors chemical synthesis
Pyrimidines chemical synthesis
Structure-Activity Relationship
Casein Kinase II antagonists & inhibitors
Casein Kinase II metabolism
Protein Kinase Inhibitors chemistry
Protein Kinase Inhibitors pharmacology
Pyrimidines chemistry
Pyrimidines pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1768-3254
- Volume :
- 46
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- European journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 21276643
- Full Text :
- https://doi.org/10.1016/j.ejmech.2010.12.025