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

Authors
  • Suzuki, Yamato
  • Cluzeau, Jérôme
  • Hara, Takafumi
  • Hirasawa, Akira
  • Tsujimoto, Gozoh
  • Oishi, Shinya
  • Ohno, Hiroaki
  • Fujii, Nobutaka
Type
Published Article
Journal
Archiv der Pharmazie
Publication Date
Sep 01, 2008
Volume
341
Issue
9
Pages
554–561
Identifiers
DOI: 10.1002/ardp.200700269
PMID: 18763715
Source
Medline
License
Unknown

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.

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