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Development of dual casein kinase 1delta/1epsilon (CK1delta/epsilon) inhibitors for treatment of breast cancer
Casein kinase 1delta/epsilon 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 CK1delta/epsilon 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.
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Piperidine | C5H2062N – PubChem