60770-00-5Relevant articles and documents
Synthesis, biological evaluation and molecular modeling studies of Schiff bases derived from 4-methylsalicylic acid as potential immunosuppressive agents
Yan, Ru,Liu, Peng-Gang,Zhang, Zhi-Ming,Fang, Xian-Ying,Zhang, Xue-Wei,Deng, Jia-Li,Zhu, Hai-Liang
, p. 5707 - 5716 (2013)
A series of Schiff bases derived from 4-methylsalicylic acid (4a-4s) were synthesized, 14 of which (4a-4h, 4j-4l, 4n, 4q, and 4s) were reported for the first time. All the synthesized compounds were evaluated for their immunosuppressive activities for the
Containing 2 - mercapto acetophenone 1, 3, 4 - oxadiazole derivative and its preparation and anti-tumor activity
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Paragraph 0028; 0029; 0030; 0043; 0044; 0045, (2017/08/25)
The invention relates to a 2-mercaptoacetophenone-containing 1, 3, 4-oxadiazole derivative, which is characterized by having a general formula as the following. In the formula, R1 represents the following, and R2 represents -H -Br. The 2-mercaptoacetophen
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.