2. Academic Validation
  3. Development of highly selective casein kinase 1δ/1ε (CK1δ/ε) inhibitors with potent antiproliferative properties

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

  • Bioorg Med Chem Lett. 2013 Aug 1;23(15):4374-80. doi: 10.1016/j.bmcl.2013.05.075.
Mathieu Bibian 1,  Ronald J Rahaim,  Jun Yong Choi,  Yoshihiko Noguchi,  Stephan Schürer,  Weimin Chen,  Shima Nakanishi,  Konstantin Licht,  Laura H Rosenberg,  Lin Li,  Yangbo Feng,  Michael D Cameron,  Derek R Duckett,  John L Cleveland,  William R Roush
Affiliations

Affiliation

  • 1 Department of Chemistry, Scripps Florida, 130 Scripps Way, Jupiter, FL 33458, United States.
PMID: 23787102 DOI: 10.1016/j.bmcl.2013.05.075
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 ≤ 50 nM versus CK1δ. The two lead compounds have ≤100 nM EC50 values in MTT assays against the human A375 melanoma cell line and have physical, in vitro and in vivo PK properties suitable for use in proof of principle animal xenograft studies against human Cancer cell lines.

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