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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
Author(s) -
Suzuki Yamato,
Cluzeau Jérôme,
Hara Takafumi,
Hirasawa Akira,
Tsujimoto Gozoh,
Oishi Shinya,
Ohno Hiroaki,
Fujii Nobutaka
Publication year - 2008
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200700269
Subject(s) - pyrazine , chemistry , pyrimidine , aniline , structure–activity relationship , acetic acid , stereochemistry , chemical synthesis , combinatorial chemistry , organic chemistry , in vitro , biochemistry
Structually related to the known CK2 inhibitors, 2,6‐disubstituted pyrazine and 4,6‐disubstituted pyrimidine derivatives were synthesized and their inhibitory activities toward CK2α and CK2α′ 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.