Electric Literature of 886-86-2, As a society publisher, everything we do is to support the scientific community – so you can trust us to always act in your best interests, and get your work the international recognition that it deserves. 886-86-2, Name is Ethyl 3-aminobenzoate methanesulfonate, SMILES is O=C(OCC)C1=CC=CC(N)=C1.CS(=O)(O)=O, belongs to phthalazine compound. In a article, author is El-Adl, Khaled, introduce new discover of the category.
In accordance with the significant impetus of the discovery of potent vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors, herein, we report the design, synthesis, and anticancer evaluation of 12 new N-substituted-4-phenylphthalazin-1-amine derivatives against HepG2, HCT-116, and MCF-7 cells as VEGFR-2 inhibitors. The results of the cytotoxicity investigation indicated that HCT-116 and MCF-7 were the most sensitive cell lines to the influence of the newly synthesized derivatives. In particular, compound 7a was found to be the most potent derivative among all the tested compounds against the three cancer cell lines, HepG2, HCT116, and MCF-7, with IC50 = 13.67 +/- 1.2, 5.48 +/- 0.4, and 7.34 +/- 0.6 mu M, respectively, which is nearly equipotent to that of sorafenib (IC50 = 9.18 +/- 0.6, 5.47 +/- 0.3, and 7.26 +/- 0.3 mu M, respectively). All synthesized derivatives, 4a,b-8a-c, were evaluated for their inhibitory activities against VEGFR-2. The tested compounds displayed high to low inhibitory activity, with IC50 values ranging from 0.14 +/- 0.02 to 9.54 +/- 0.85 mu M. Among them, compound 7a was found to be the most potent derivative that inhibited VEGFR-2 at an IC50 value of 0.14 +/- 0.02 mu M, which is nearly 72% of that of the sorafenib IC50 value (0.10 +/- 0.02 mu M). Compounds 7b, 8c, 8b, and 8a exhibited very good activity with IC50 values of 0.18 +/- 0.02, 0.21 +/- 0.03, 0.24 +/- 0.02, and 0.35 +/- 0.04 mu M, respectively. Molecular modeling studies were carried out for all compounds against the VEGFR-2 active site. The data obtained from biological testing highly correlated with that obtained from molecular modeling studies. However, these modifications led to new phthalazine derivatives with higher VEGFR-2 inhibitory activities than vatalanib and which are nearly equipotent to sorafenib.
Electric Literature of 886-86-2, Because enzymes can increase reaction rates by enormous factors and tend to be very specific, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about 886-86-2.
Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem