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

…, VG Bdzhola, NV Briukhovetska, AO Balanda…

文献索引：Golub, Andriy G.; Bdzhola, Volodymyr G.; Briukhovetska, Nadiia V.; Balanda, Anatoliy O.; Kukharenko, Olexander P.; Kotey, Igor M.; Ostrynska, Olga V.; Yarmoluk, Sergiy M. European Journal of Medicinal Chemistry, 2011 , vol. 46, # 3 p. 870 - 876

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被引用次数: 39

摘要

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 ...