One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, name: 5-Methylbenzo[d]oxazole-2(3H)-thione, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 22876-22-8, Name is 5-Methylbenzo[d]oxazole-2(3H)-thione, molecular formula is C8H7NOS
Design, synthesis, molecular docking, and anticancer activity of benzoxazole derivatives as VEGFR-2 inhibitors
Novel series of benzoxazoles 4a-f-16 were designed, synthesized, and evaluated for anticancer activity against HepG2, HCT-116, and MCF-7 cells. HCT-116 was the most sensitive cell line to the influence of the new derivatives. In particular, compound 5e was found to be the most potent against HepG2, HCT-116, and MCF-7 with IC50 = 4.13 ¡À 0.2, 6.93 ¡À 0.3, and 8.67 ¡À 0.5 muM, respectively. Compounds 5c, 5f, 6b, 5d, and 6c showed the highest anticancer activities against HepG2 cells with IC50 of 5.93 ¡À 0.2, 6.58 ¡À 0.4, 8.10 ¡À 0.7, 8.75 ¡À 0.7, and 9.95 ¡À 0.9 muM, respectively; HCT-116 cells with IC50 of 7.14 ¡À 0.4, 9.10 ¡À 0.8, 7.91 ¡À 0.6, 9.52 ¡À 0.5, and 12.48 ¡À 1.1 muM, respectively; and MCF-7 cells with IC50 of 8.93 ¡À 0.6, 10.11 ¡À 0.9, 12.31 ¡À 1.0, 9.95 ¡À 0.8, and 15.70 ¡À 1.4 muM, respectively, compared with sorafenib as a reference drug with IC50 of 9.18 ¡À 0.6, 5.47 ¡À 0.3, and 7.26 ¡À 0.3 muM, respectively. The most active compounds 5c-f and 6b,c were further evaluated for their vascular endothelial growth factor receptor-2 (VEGFR-2) inhibition. Compounds 5e and 5c potently inhibited VEGFR-2 at lower IC50 values of 0.07 ¡À 0.01 and 0.08 ¡À 0.01 muM, respectively, compared with sorafenib (IC50 = 0.1 ¡À 0.02 muM). Compound 5f potently inhibited VEGFR-2 at low IC50 value (0.10 ¡À 0.02 muM) equipotent to sorafenib. Our design was based on the essential pharmacophoric features of the VEGFR-2 inhibitor sorafenib. Molecular docking was performed for all compounds to assess their binding pattern and affinity toward the VEGFR-2 active site.
Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. name: 5-Methylbenzo[d]oxazole-2(3H)-thione, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 22876-22-8, in my other articles.
Reference£º
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem