Discovery and structure–activity relationship of 2, 6-disubstituted pyrazines, potent and selective inhibitors of protein kinase CK2

…, K Suyama, H Ueda, S Yamaguchi, K Nishimura…

文献索引：Fuchi, Nobuhiro; Iura, Yosuke; Kaneko, Hiroaki; Nitta, Aiko; Suyama, Kazuharu; Ueda, Hiroshi; Yamaguchi, Shinichi; Nishimura, Kazumi; Fujii, Shigeo; Sekiya, Yumiko; Yamada, Masateru; Takahashi, Toshiya Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 13 p. 4358 - 4361

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被引用次数: 10

摘要

We report the discovery and structure–activity relationship of 2, 6-disubstituted pyrazines, which are potent and selective CK2 inhibitors. Lead compound 1 was identified, and derivatives were prepared to develop potent inhibitory activity. As a result, we obtained compound 7, which was the smallest unit that retained potency. Then, introducing an aminoalkyl group at the 6-position of the indazole ring resulted in improved efficacy in ...