1454585-06-8Relevant academic research and scientific papers
Development of dual casein kinase 1δ/1ε (CK1δ/ε) inhibitors for treatment of breast cancer
Monastyrskyi, Andrii,Nilchan, Napon,Quereda, Victor,Noguchi, Yoshihiko,Ruiz, Claudia,Grant, Wayne,Cameron, Michael,Duckett, Derek,Roush, William
, p. 590 - 602 (2018/01/01)
Casein kinase 1δ/ε have been identified as promising therapeutic target for oncology application, including breast and brain cancer. Here, we described our continued efforts in optimization of a lead series of purine scaffold inhibitors that led to identification of two new CK1δ/ε inhibitors 17 and 28 displaying low nanomolar values in antiproliferative assays against the human MDA-MB-231 triple negative breast cancer cell line and have physical, in vitro and in vivo pharmacokinetic properties suitable for use in proof of principle animal xenograft studies against human cancers.
WEE1 DEGRADATION INHIBITORS
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Page/Page column 80, (2013/09/12)
The invention provides compounds that inhibit the degradation of Weel. The compounds of the present invention are generally N-((1H-benzo[d]imidazol-2- yl)methyl)-9H-purin-6-amines. Compounds of the invention can be used for treatment of malconditions in p
Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties
Bibian, Mathieu,Rahaim, Ronald J.,Choi, Jun Yong,Noguchi, Yoshihiko,Schürer, 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.
, p. 4374 - 4380 (2013/07/26)
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 kinas
