Literature DB >> 18763715

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

Yamato Suzuki1, Jérôme Cluzeau, Takafumi Hara, Akira Hirasawa, Gozoh Tsujimoto, Shinya Oishi, Hiroaki Ohno, Nobutaka Fujii.   

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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Year:  2008        PMID： 18763715     DOI： 10.1002/ardp.200700269

Source DB:  PubMed          Journal:  Arch Pharm (Weinheim)        ISSN： 0365-6233            Impact factor:   3.751


  3 in total

1.  A detailed thermodynamic profile of cyclopentyl and isopropyl derivatives binding to CK2 kinase.

Authors:  Takayoshi Kinoshita; Yusuke Sekiguchi; Harumi Fukada; Tetsuko Nakaniwa; Toshiji Tada; Shinya Nakamura; Kazuo Kitaura; Hiroaki Ohno; Yamato Suzuki; Akira Hirasawa; Isao Nakanishi; Gozoh Tsujimoto
Journal:  Mol Cell Biochem       Date:  2011-07-07       Impact factor: 3.396

2.  Structure of human protein kinase CK2 alpha 2 with a potent indazole-derivative inhibitor.

Authors:  Tetsuko Nakaniwa; Takayoshi Kinoshita; Yusuke Sekiguchi; Toshiji Tada; Isao Nakanishi; Kazuo Kitaura; Yamato Suzuki; Hiroaki Ohno; Akira Hirasawa; Gozoh Tsujimoto
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2009-01-31

3.  Crystal structure of human CK2α at 1.06 Å resolution.

Authors:  Takayoshi Kinoshita; Tetsuko Nakaniwa; Yusuke Sekiguchi; Yuri Sogabe; Atsushi Sakurai; Shinya Nakamura; Isao Nakanishi
Journal:  J Synchrotron Radiat       Date:  2013-10-02       Impact factor: 2.616
  3 in total

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