Sanad, Sherif M. H. published the artcileTandem synthesis, cytotoxicity, and in silico study of new 1,3,4-oxadiazoles as potential thymidylate synthase inhibitors, Recommanded Product: Sodium chloro(tosyl)amide trihydrate, the publication is Archiv der Pharmazie (Weinheim, Germany), database is CAplus and MEDLINE.
A new series of pyrrole-linked mono- and bis(1,3,4-oxadiazole) hybrids I [R = H, Me, Cl, etc.] and II [R1 = -PhO(CH2)2OPh-, -PhO(CH2)3OPh-, -PhO(CH2)4OPh-, etc.], attached to various arene units, was prepared using a two-step tandem protocol. Therefore, a benzohydrazide derivative was condensed with the appropriate aldehydes RCHO in ethanol at 80°C for 60-150 min to give the corresponding N-(benzoylhydrazones). Without isolation, the previous intermediates underwent intramol. oxidative cyclization in DMSO at 180°C for 90-200 min in the presence of chloramine trihydrate to afford the target hybrids I. The cytotoxicity of all hybrids was examined in vitro against the MCF-7, HEPG2 and Caco2 cell lines. Arene-linked hybrids I [R = NO2, 4-acetoxy], were the most potent ones, with IC50 values ranging from 5.47 to 8.80 and 12.75 to 21.22 μM, resp., when tested on the above cell lines. At the tested concentrations of 5 and 7.5 μM, hybrid I [R = 4-nitro] inhibited thymidylate synthase (TS) with the best inhibition percentages of 72.3 and 91.3, whereas hybrid I [R = 4-acetoxy] displayed comparable inhibitory activity to the reference pemetrexed. Hybrid I [R = 4-acetoxy] had inhibition percentages of 62.7 and 82.6, whereas pemetrexed had inhibition percentages of 59.2 and 80.2, resp. The capability of hybrids I [R = 4-nitro, 4-acetoxy] as potential TS inhibitors was supported by mol. docking studies, while SwissADME predicts their efficacy as drug-like scaffolds.
Archiv der Pharmazie (Weinheim, Germany) published new progress about 7080-50-4. 7080-50-4 belongs to chlorides-buliding-blocks, auxiliary class Halogenation Reagent,Inhibitor, name is Sodium chloro(tosyl)amide trihydrate, and the molecular formula is C7H13ClNNaO5S, Recommanded Product: Sodium chloro(tosyl)amide trihydrate.
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