Synthesis and structure-activity relationship of trisubstituted thiazoles as Cdc7 kinase inhibitors
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.
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.
p. 364 - 382
(2014/05/20)
Concise syntheses of meridianins and meriolins using a catalytic domino amino-palladation reaction
A synthesis of natural and synthetic members of the meridianin family of kinase inhibitory natural products has been developed. The sequence utilizes a variation of the Cacchi palladium-catalyzed domino reaction to efficiently construct the heterocyclic f
Walker, Scott R.,Czyz, Milena L.,Morris, Jonathan C.
supporting information
p. 708 - 711
(2014/03/21)
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