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Synthesis and structure–activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors

…, G Yao, H Shu, MR Kaller, JG Allen, MF Weidner…

文献索引:Reichelt, Andreas; Bailis, Julie M.; Bartberger, Michael D.; Yao, Guomin; Shu, Hong; Kaller, Matthew R.; Allen, John G.; Weidner, Margaret F.; Keegan, Kathleen S.; Dao, Jennifer H. European Journal of Medicinal Chemistry, 2014 , vol. 80, p. 364 - 382

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被引用次数: 7

摘要

Abstract The Cell division cycle 7 (Cdc7) protein kinase is essential for DNA replication and maintenance of genome stability. We systematically explored thiazole-based compounds as inhibitors of Cdc7 kinase activity in cancer cells. Our studies resulted in the identification of a potent, selective Cdc7 inhibitor that decreased phosphorylation of the direct substrate MCM2 in vitro and in vivo, and inhibited DNA synthesis and cell viability in vitro.