title: Synthesis and biological evaluation of 3-(substituted-benzylidene)-1,3-dihydro-indolin derivatives as human protein kinase CK2 and p60(c-Src) tyrosine kinase inhibitors.
abstract: Human protein kinase CK2 is an ubiquitous serine/threonine kinase that is typically found in tetrameric complexes consisting of two catalytic (alpha and/or alpha') and two regulatory beta 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)-1,3-dihydro-indolin-2-thione derivatives are more effective than indolin-2-one congeners for the inhibition of CK2 and p60(c-Src) tyrosine kinase.
authors.affiliation: University of Ankara, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Turkey. olgen@pharmacy.ankara.edu.tr
authors.forename: Süreyya
authors.initials: S
authors.lastname: Olgen
authors.forename: Claudia
authors.initials: C
authors.lastname: Götz
authors.forename: Joachim
authors.initials: J
authors.lastname: Jose
mesh_terms: D001597:Benzylidene Compounds / Q000737:chemistry*; D047390:Casein Kinase II / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism; D005069:Evaluation Studies as Topic; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D047428:Protein Kinase Inhibitors / Q000494:pharmacology*; D016392:Proto-Oncogene Proteins pp60(c-src) / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011994:Recombinant Proteins / Q000037:antagonists & inhibitors; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D001597:Benzylidene Compounds; D007211:Indoles; D047428:Protein Kinase Inhibitors; D011994:Recombinant Proteins; D016392:Proto-Oncogene Proteins pp60(c-src); D047390:Casein Kinase II