16952-66-2Relevant articles and documents
Novel 1,3,4-oxadiazole thioether derivatives targeting thymidylate synthase as dual anticancer/antimicrobial agents
Du, Qian-Ru,Li, Dong-Dong,Pi, Ya-Zhou,Li, Jing-Ran,Sun, Jian,Fang, Fei,Zhong, Wei-Qing,Gong, Hai-Bin,Zhu, Hai-Liang
, p. 2286 - 2297 (2013/05/09)
A series of novel 1,3,4-oxadiazole thioether derivatives (compounds 9-44) were designed and synthesized as potential inhibitors of thymidylate synthase (TS) and as anticancer agents. The in vitro anticancer activities of these compounds were evaluated against three cancer cell lines by the MTT method. Among all the designed compounds, compound 18 bearing a nitro substituent exhibited more potent in vitro anticancer activities with IC50 values of 0.7 ± 0.2, 30.0 ± 1.2, 18.3 ± 1.4 μM, respectively, which was superior to the positive control. In the further study, it was identified as the most potent inhibitor against two kinds of TS protein (for human TS and Escherichia coli TS, IC50 values: 0.62 and 0.47 μM, respectively) in the TS inhibition assay in vitro and the most potent antibacterial agents with MIC (minimum inhibitory concentrations) of 1.56-3.13 μg/mL against the tested four bacterial strains. Molecular docking and 3D-QSAR study supported that compound 18 can be selected as dual antitumor/antibacterial candidate in the future study.
9-Cyano-1-azapaullone (Cazpaullone), a Glycogen Synthase Kinase-3 (GSK-3) inhibitor activating pancreatic β cell protection and replication
Stukenbrock, Hendrik,Mussmann, Rainer,Geese, Marcus,Ferandin, Yoan,Lozach, Olivier,Lemcke, Thomas,Kegel, Simone,Lomow, Alexander,Burk, Ulrike,Dohrmann, Cord,Meijer, Laurent,Austen, Matthias,Kunick, Conrad
, p. 2196 - 2207 (2008/12/22)
Recently, the serine/threonine kinase glycogen synthase kinase-3 (GSK-3) emerged as a regulator of pancreatic β cell growth and survival. On the basis of the previous observation that GSK-3 inhibitors like 1-azakenpaullone promote β cell protection and re
Facile synthesis of functionalized 4-aminopyridines
Nishiwaki, Nagatoshi,Azuma, Mayumi,Tamura, Mina,Hori, Kazushige,Tohda, Yasuo,Ariga, Masahiro
, p. 2170 - 2171 (2007/10/03)
The title compounds are readily available by ring transformation of nitropyrimidinone with active methylene compounds in the presence of ammonium acetate.