《Identification of 1,3-thiazole-5-carboxylic Acid Derivatives as Inhibitors of Protein Kinase CK2》 was written by Protopopov, Mykola V.; Volynets, Galyna P.; Starosyla, Sergiy A.; Vdovin, Vasyl S.; Lukashov, Sergiy S.; Bilokin, Yaroslav V.; Bdzhola, Volodymyr G.; Yarmoluk, Sergiy M.. Application In Synthesis of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid And the article was included in Current Enzyme Inhibition on August 31 ,2018. The article conveys some information:
Serine/threonine protein kinase CK2 is involved in the regulation of a number of cellular functions such as cell growth, proliferation, differentiation and apoptosis. Increased activity of CK2 is associated with the development of different types of cancer, inflammatory response, pain and virus infections. Therefore, protein kinase CK2 is an attractive mol. target for the development of small-mol. inhibitors which can be important compounds for pharmaceutical application. The main aim of this research is to identify novel chem. class of CK2 inhibitors with good lead-like properties. In order to find novel CK2 inhibitors, virtual screening experiments were performed using Autodock software. Best-scored compounds were tested in vitro using P32 radioactive kinase assay. Small-mol. inhibitors of protein kinase CK2 were identified among the derivatives of 1,3-thiazole-5-carboxylic acid. The most active compound inhibited CK2 with IC50 value of 0.4 μM. Ligand efficiency for studied derivatives of 1,3-thiazole-5-carboxylic acid was in the range from 0.45 to 0.56 kcal/mol/non-hydrogen atom. Considering the fact that the lower limit for ligand efficiency parameter is 0.3, the identified CK2 inhibitors among the derivatives of 1,3-thiazole-5-carboxylic acid are excellent candidates for further lead optimization. The results came from multiple reactions, including the reaction of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0Application In Synthesis of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid)
4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid(cas: 144060-98-0) belongs to pyridine. Pyridine-based materials are valued for their optical and physical properties as well as their medical potential. Additionally, pyridine-based natural products continue to be discovered and studied for their properties and to understand their biosynthesis.Application In Synthesis of 4-Methyl-2-(pyridin-4-yl)thiazole-5-carboxylic acid
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica