2. Academic Validation
  3. Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2

Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin-4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2

  • Eur J Med Chem. 2011 Mar;46(3):870-6. doi: 10.1016/j.ejmech.2010.12.025.
Andriy G Golub 1,  Volodymyr G Bdzhola,  Nadiia V Briukhovetska,  Anatoliy O Balanda,  Olexander P Kukharenko,  Igor M Kotey,  Olga V Ostrynska,  Sergiy M Yarmoluk
Affiliations

Affiliation

  • 1 Department of Combinatorial Chemistry, Institute of Molecular Biology and Genetics of the National Academy of Sciences of Ukraine,150 Zabolotnogo Street, 03143 Kyiv, Ukraine. [email protected]
PMID: 21276643 DOI: 10.1016/j.ejmech.2010.12.025
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.

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