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
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.