Synthesis and Biological Evaluation of 3-(Substituted-benzylidene)-l,3-dihydro-indolin Derivatives as Human Protein Kinase CK2 and p60^<c-Src> Tyrosine Kinase Inhibitors(Medicinal Chemistry)
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概要
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Human protein kinase CK2 is an ubiquitous serine/threonine kinase that is typically found in tetrameric complexes consisting of two catalytic (α and/or α') and two regulatory β subunits. Although there is growing evidence that besides the participation of CK2 in a complex series of cellular functions, this protein kinase is involved in cell viability, cell proliferation, and neoplastic transformation. In the present study, a series of 3-(substituted-benzylidene)-1,3-dihydro-indolin-2-thione derivatives and the corresponding indolin-2-one congeners were tested for their inhibition of human recombinant protein kinase CK2 in vitro. The efficacy of these compounds was compared with their inhibitory results of p60^<c-Src> tyrosine kinase. It was found that 3-(substituted-benzylidene)-l13-dihydro-mdolm-2-thione derivatives are more effective than indolin-2-one congeners for the inhibition of CK2 and p60^<c-Src> tyrosine kinase.
- 公益社団法人日本薬学会の論文
- 2007-04-01
著者
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Olgen Sureyya
University Of Ankara Faculty Of Pharmacy Department Of Pharmaceutical Chemistry
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Gotz Claudia
Medicinal Biochemistry And Molecular Biology Saarland University
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JOSE Joachim
Bioanalytics, Institute for Pharmaceutical and Medicinal Chemistry, Heinrich-Heine-University
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Jose Joachim
Bioanalytics Institute For Pharmaceutical And Medicinal Chemistry Heinrich-heine-university