Structure-activity relationships of pyrazine-based CK2 inhibitors: synthesis and evaluation of 2,6-disubstituted pyrazines and 4,6-disubstituted pyrimidines

Arch Pharm (Weinheim). 2008 Sep;341(9):554-61. doi: 10.1002/ardp.200700269.

Abstract

Structurally related to the known CK2 inhibitors, 2,6-disubstituted pyrazine and 4,6-disubstituted pyrimidine derivatives were synthesized and their inhibitory activities toward CK2alpha and CK2alpha' were evaluated. Structure-activity relationship study has revealed that several pyrazine derivatives bearing a (pyrrol-3-yl)acetic acid and a monosubstituted aniline possess potent inhibitory activities.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Casein Kinase II / antagonists & inhibitors*
  • Enzyme Inhibitors / chemical synthesis*
  • Enzyme Inhibitors / pharmacology*
  • Indicators and Reagents
  • Pyrazines / chemical synthesis*
  • Pyrazines / pharmacology*
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Enzyme Inhibitors
  • Indicators and Reagents
  • Pyrazines
  • Pyrimidines
  • Casein Kinase II