A catalyst don’t appear in the overall stoichiometry of the reaction it catalyzes, but it must appear in at least one of the elementary reactions in the mechanism for the catalyzed reaction. 31618-90-3, Name is (Diethoxyphosphoryl)methyl 4-methylbenzenesulfonate, molecular formula is C12H19O6PS. In an article, author is El-Adl, Khaled,once mentioned of 31618-90-3, Product Details of 31618-90-3.
N-Substituted-4-phenylphthalazin-1-amine-derived VEGFR-2 inhibitors: Design, synthesis, molecular docking, and anticancer evaluation studies
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.
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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem