Synthesis and biological evaluation of substituted (thieno[2,3-d]pyrimidin- 4-ylthio)carboxylic acids as inhibitors of human protein kinase CK2
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.
Golub, Andriy G.,Bdzhola, Volodymyr G.,Briukhovetska, Nadiia V.,Balanda, Anatoliy O.,Kukharenko, Olexander P.,Kotey, Igor M.,Ostrynska, Olga V.,Yarmoluk, Sergiy M.
scheme or table
p. 870 - 876
(2011/04/22)
Synthesis and application of some new thienopyrimidine derivatives as antimicrobial agents
The paper describes the synthesis of a new ring system 5-phenylthieno[2,3-d]pyrimidine-4(3H)one (2). Chlorination of (2) with PCl5, POCl3 gave the corresponding 4-chloro derivative (4). Several derivatives of the latter compound have been synthesised and tested for antimicrobial activity.
Hozien,Atta,Hassan,Abdel-Wahab,Ahmed
p. 3733 - 3755
(2007/10/03)
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