Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide--potential inhibitors of human protein kinase CK2

Andzelika Najda-Bernatowicz; Maja Łebska; Andrzej Orzeszko; Katarzyna Kopańska; Ewa Krzywińska; Grazyna Muszyńska; Maria Bretner

doi:10.1016/j.bmc.2008.12.071

Synthesis of new analogs of benzotriazole, benzimidazole and phthalimide--potential inhibitors of human protein kinase CK2

Bioorg Med Chem. 2009 Feb 15;17(4):1573-8. doi: 10.1016/j.bmc.2008.12.071. Epub 2009 Jan 7.

Authors

Andzelika Najda-Bernatowicz¹, Maja Łebska, Andrzej Orzeszko, Katarzyna Kopańska, Ewa Krzywińska, Grazyna Muszyńska, Maria Bretner

Affiliation

¹ Institute of Biochemistry and Biophysics, Warsaw, Poland.

PMID: 19168362
DOI: 10.1016/j.bmc.2008.12.071

Abstract

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Benzimidazoles / chemical synthesis*
Benzimidazoles / pharmacology
Casein Kinase II / antagonists & inhibitors*
Casein Kinase II / metabolism
Humans
Phthalimides / chemical synthesis*
Phthalimides / pharmacology
Protein Kinase Inhibitors / chemical synthesis*
Protein Kinase Inhibitors / pharmacology
Structure-Activity Relationship
Triazoles / chemical synthesis*
Triazoles / pharmacology

Substances

Benzimidazoles
Phthalimides
Protein Kinase Inhibitors
Triazoles
benzotriazole
Casein Kinase II