Synthesis and evaluation of pyrido-thieno-pyrimidines as potent and selective Cdc7 kinase inhibitors

…, C Tovar, X Yin, Q Xu, IT Todorov, LT Vassilev…

Index: Zhao, Chunlin; Tovar, Christian; Yin, Xuefeng; Xu, Qui; Todorov, Ivan T.; Vassilev, Lyubomir T.; Chen, Li Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 2 p. 319 - 323

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Citation Number: 42

Abstract

Cdc7 kinase plays a critical role in the regulation of DNA replication in eukaryotic cells and has been proposed as a target for cancer therapy. We have identified a class of Cdc7/Dbf4 inhibitors with a pyrido-thieno-pyrimidine core structure. Synthesis of a focused pyrido- thieno-pyrimidine library yielded potent and selective Cdc7 inhibitors with antiproliferative activity against cancer cells in vitro. Their synthesis and SAR data are presented herein.