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

Add time:08/01/2019    Source:sciencedirect.com

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 (IC50 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.

► Thienopyrimidines are novel and potent class of protein kinase CK2 inhibitors. ► Thienopyrimidines display selectivity towards CK2 and ATP-competitive type of inhibition. ► Key role in the structure of thienopyrimidine CK2 inhibitors plays carboxyl group.

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