Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide--potential inhibitors of human protein kinase CK2.
New derivatives of 4,5,6,7-tetrabromo-1H-1,2,3-benzotriazole (TBBt), 4,5,6,7-tetrabromo-1H-benzimidazole (TBBi), and N-substituted tetrabromophthalimides were synthesized and their effect on the activity of human protein kinase CK2 was examined. The most active were derivatives with N-hydroxypropyl substituents (IC(50) in 0.32-0.54 microM range) whereas derivatives of phthalimide were almost ineffective.
Najda-Bernatowicz
Andzelika
A
Institute of Biochemistry and Biophysics, Warsaw, Poland.
Łebska
Maja
M
Orzeszko
Andrzej
A
Kopańska
Katarzyna
K
Krzywińska
Ewa
E
Muszyńska
Grazyna
G
Bretner
Maria
M
D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D047390:Casein Kinase II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D010797:Phthalimides / Q000138:chemical synthesis* / Q000494:pharmacology; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D001562:Benzimidazoles; D010797:Phthalimides; D047428:Protein Kinase Inhibitors; D014230:Triazoles; C012771:benzotriazole; D047390:Casein Kinase II