Patterson, Jaclyn R.; Graves, Alan P.; Stoy, Patrick; Cheung, Mui; Desai, Tina A.; Fries, Harvey; Gatto, Gregory J. Jr.; Holt, Dennis A.; Shewchuk, Lisa; Totoritis, Rachel; Wang, Liping; Kallander, Lara S. published their research in Journal of Medicinal Chemistry in 2021. The article was titled 《Identification of Diarylurea Inhibitors of the Cardiac-Specific Kinase TNNI3K by Designing Selectivity Against VEGFR2, p38α, and B-Raf》.Product Details of 3934-20-1 The article contains the following contents:
A series of diarylurea inhibitors of the cardiac-specific kinase TNNI3K were developed to elucidate the biol. function of TNNI3K and evaluate TNNI3K as a therapeutic target for the treatment of cardiovascular diseases. Utilizing a structure-based design, enhancements in kinase selectivity were engineered into the series, capitalizing on the established X-ray crystal structures of TNNI3K, VEGFR2, p38α, and B-Raf. Our efforts culminated in the discovery of an in vivo tool compound 47 (GSK329), which exhibited desirable TNNI3K potency and rat pharmacokinetic properties as well as promising kinase selectivity against VEGFR2 (40-fold), p38α (80-fold), and B-Raf (>200-fold). Compound 47 demonstrated pos. cardioprotective outcomes in a mouse model of ischemia/reperfusion cardiac injury, indicating that optimized exemplars from this series, such as 47, are favorable leads for discovering novel medicines for cardiac diseases. In addition to this study using 2,4-Dichloropyrimidine, there are many other studies that have used 2,4-Dichloropyrimidine(cas: 3934-20-1Product Details of 3934-20-1) was used in this study.
2,4-Dichloropyrimidine(cas: 3934-20-1) is a member of organic chlorides. Organic chloride content in crude oil can be detected through specialized laboratory analysis. Care and attention are essential while sampling and testing.Product Details of 3934-20-1
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia