In 2022,Powell, Chelsea E.; Hatcher, John M.; Jiang, Jie; Vatsan, Prasanna S.; Che, Jianwei; Gray, Nathanael S. published an article in ACS Medicinal Chemistry Letters. The title of the article was 《Selective Macrocyclic Inhibitors of DYRK1A/B》.Related Products of 14660-52-7 The author mentioned the following in the article:
Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase 1A (DYRK1A) is a therapeutic target of interest due to the roles it plays in both neurol. diseases and cancer. We present the development of the first macrocyclic inhibitors of DYRK1A. Initial lead inhibitor JH-XIV-68-3 (3) displayed selectivity for DYRK1A and close family member DYRK1B in biochem. and cellular assays, and demonstrated antitumor efficacy in head and neck squamous cell carcinoma (HNSCC) cell lines. However, we noted that it suffered from rapid aldehyde oxidase (AO)-mediated metabolism To overcome this liability, we generated a derivative (JH-XVII-10 (10)), where fluorine was introduced to block the 2-position of the azaindole and render the mol. resistant to AO activity. We showed that 10 maintains remarkable potency and selectivity in biochem. and cellular assays as well as antitumor efficacy in HNSCC cell lines and improved metabolic stability. Therefore, 10 represents a promising new scaffold for developing DYRK1A-targeting chem. probes and therapeutics.Ethyl 5-bromovalerate(cas: 14660-52-7Related Products of 14660-52-7) was used in this study.
Ethyl 5-bromovalerate(cas: 14660-52-7) belongs to bromides. A variety of minor organobromine compounds are found in nature, but none are biosynthesized or required by mammals. Organobromine compounds have fallen under increased scrutiny for their environmental impact.Related Products of 14660-52-7
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary