Application of 1821-12-1, Enzymes are biological catalysts that produce large increases in reaction rates and tend to be specific for certain reactants and products. 1821-12-1, Name is 4-Phenylbutanoic acid, SMILES is O=C(O)CCCC1=CC=CC=C1, belongs to phthalazines compound. In a article, author is El-Helby, Abdel-Ghany A., introduce new discover of the category.
Design, Synthesis, Molecular Docking, and Anticancer Activity of Phthalazine Derivatives as VEGFR-2 Inhibitors
Novel series of phthalazine derivatives 6-11 were designed, synthesized, and evaluated for their anticancer activity against two human tumor cell lines, HCT-116 human colon adenocarcinoma and MCF-7 breast cancer cells, targeting the VEGFR-2 enzyme. Compounds 7a,b and 8b,c showed the highest anticancer activities against both HCT116 human colon adenocarcinoma cells with IC50 of 6.04 +/- 0.30, 13.22 +/- 0.22, 18 +/- 0.20, and 35 +/- 0.45M, respectively, and MCF-7 breast cancer cells with IC50 of 8.8 +/- 0.45, 17.9 +/- 0.50, 25.2 +/- 0.55, and 44.3 +/- 0.49M, respectively, in comparison to sorafenib as reference drug with IC50 of 5.47 +/- 0.3 and 7.26 +/- 0.3M, respectively. Eleven compounds in this series were further evaluated for their inhibitory activity against VEGFR-2, where compounds 7a, 7b, 8c, and 8b also showed the highest VEGFR-2 inhibition with IC50 of 0.11 +/- 0.01, 0.31 +/- 0.03, 0.72 +/- 0.08, and 0.91 +/- 0.08M, respectively, in comparison to sorafenib as reference ligand with IC50 of 0.1 +/- 0.02. Furthermore, molecular docking studies were performed for all synthesized compounds to predict their binding pattern and affinity towards the VEGFR-2 active site, in order to rationalize their anticancer activity in a qualitative way.
Application of 1821-12-1, The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 1821-12-1 is helpful to your research.
Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem