Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties

…, Y Noguchi, S Schürer, W Chen, S Nakanishi…

Index: Bibian, Mathieu; Rahaim, Ronald J.; Choi, Jun Yong; Noguchi, Yoshihiko; Schuerer, Stephan; Chen, Weimin; Nakanishi, Shima; Licht, Konstantin; Rosenberg, Laura H.; Li, Lin; Feng, Yangbo; Cameron, Michael D.; Duckett, Derek R.; Cleveland, John L.; Roush, William R. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 15 p. 4374 - 4380

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Citation Number: 16

Abstract

The development of a series of potent and highly selective casein kinase 1δ/ε (CK1δ/ε) inhibitors is described. Starting from a purine scaffold inhibitor (SR-653234) identified by high throughput screening, we developed a series of potent and highly kinase selective inhibitors, including SR-2890 and SR-3029, which have IC50⩽ 50nM versus CK1δ. The two lead compounds have⩽ 100nM EC50 values in MTT assays against the human A375 ...