16779-03-6Relevant articles and documents
A novel approach towards design, synthesis and evaluation of some Schiff base analogues of 2-aminopyridine and 2-aminobezothiazole against hepatocellular carcinoma
Chacko, Shinu,Samanta, Subir
, p. 162 - 176 (2017/02/26)
Hepatocellular carcinoma is the most common primary malignancy of the liver with poor prognosis. In this study novel, Schiff's bases of 2-aminopyridine (SSSC-26 to 31) and 2-aminobenzothiazole (SSSC-32 to 37) were designed, synthesised and evaluated for antioxidant potential using DPPH method, and anti-hepatocellular carcinoma property using diethylnitrosamine (DEN) induced hepatocellular carcinoma rat model. The in-silico pharmacokinetic, rule of five and toxicity studies reveals that all the leads have an excellent intrinsic quality and sufficient structural features necessary for an oral activity. Molecular docking studies of all compounds into the ligand binding pocket of checkpoint kinase1 and vascular endothelial growth factor receptor-2 was also performed using Schrodinger software suite v8.5, and which have shown good Glide scores. Further compounds were synthesised based on the docking score and ADMET profile. The 1,1-diphenyl-2-picrylhydrazil (DPPH) scavenging study was carried out, and results showed that SSSC-29 (IC50-63.60) and SSSC-33 (IC50-60.32) were having good anti-oxidant potential in comparison with ascorbic acid (IC50-55.27). SSSC-33 further evaluated for anti-cancer potential against diethylnitrosamine (200 mg/kg bw) induced hepatocellular carcinoma in rats. The biochemical, histopathological and morphological data showed that SSSC-33 can reverse the changes occurred in the cancerous liver significantly. All these findings suggested that SSSC-33-((benzo[d]thiazol-2-ylimino) methyl)phenol) could be a potential compound in combating the oxidative damage of hepatic cells occurred due to the development of hepatocellular carcinoma induced by a chemical carcinogen, DEN.
Ultrasound-assisted one-pot synthesis of bis-azetidinones in the presence of zeolite
Jetti, Venkateshwarlu,Chidurala, Praveen,Pagadala, Ramakanth,Meshram, Jyotsna S.,Ramakrishna, Chowdam
, p. E183-E188 (2014/11/08)
Sonochemical method is an innovative task for the sustainable chemical research industry. In this work, an attempt was made to synthesize bis-azetidin-2-ones (2a, 2b, 2c, 2d, 2e, 2f, 2g, 2h, 2i, 2j) by Staudinger reaction ([2 + 2] ketene-imine cycloadditi
Design of new cognition enhancers: From computer prediction to synthesis and biological evaluation
Geronikaki, Athina A.,Dearden, John C.,Filimonov, Dmitrii,Galaeva, Irina,Garibova, Taissia L.,Gloriozova, Tatiana,Krajneva, Valentina,Lagunin, Alexey,Macaev, Fliur Z.,Molodavkin, Guenadij,Poroikov, Vladimir V.,Pogrebnoi, Serghei I.,Shepeli, Felix,Voronina, Tatiana A.,Tsitlakidou, Maria,Vlad, Liudmila
, p. 2870 - 2876 (2007/10/03)
To discover new cognition enhancers, a set of virtually designed synthesizable compounds from different chemical series was investigated using two computer-aided approaches. One of the approaches is prediction of biological activity spectra for substances
