209002-03-9Relevant articles and documents
Optimization and biological evaluation of 2-aminobenzothiazole derivatives as Aurora B kinase inhibitors
Lee, Eun,An, Ying,Kwon, Junhee,Kim, Keun Il,Jeon, Raok
, p. 3614 - 3622 (2017/06/13)
A strong relationship between abnormal functions of Aurora kinases and tumorigenesis has been reported for decades. Consequently, Aurora kinases serve as potential targets for anticancer agents. Here, we identified aminobenzothiazole derivatives as novel inhibitors of Aurora B kinase through bioisosteric replacement of the previous inhibitors, aminobenzoxazole derivatives. Most of the urea-linked aminobenzothiazole derivatives showed potent and selective inhibitory activity against Aurora B kinase over Aurora A kinase. Molecular modeling indicated that compound 15g bound well to the active site of Aurora B kinase and formed the essential hydrogen bonds. The potent compounds, 15g and 15k, were selected, and their biological effects were evaluated using HeLa cell lines. It was found that these compounds inhibited the phosphorylation of histone H3 at Ser10 and induced G2/M cell cycle arrest. We suggest that the reported compounds have the potential to be further developed as anticancer therapeutics.
Highly active binuclear Cu(II) catalyst bearing an unsymmetrical bipyridine-pyrazole-amine ligand for the azide-alkyne cycloaddition reaction
Han, Baofeng,Xiao, Xiao,Wang, Lan,Ye, Wenjing,Liu, Xiaoping
, p. 1446 - 1450 (2016/10/04)
Ligands containing NH groups often show special characteristics. In this paper, a well-defined dinuclear Cu(II) complex bearing an unsymmetrical bipyridine-pyrazole-amine ligand was synthesized by the condensation of N–H to release H2O. Using sodium L-ascorbate as a reductant, the binuclear complex showed excellent activity in 1,3-dipolar cycloaddition reactions between alkynes and azides to obtain 1,4-disubstituted triazoles in 95%–99% isolated yields.
Acetylenic 1,5-diarylpyrazoles as antiinflammatory agents
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, (2008/06/13)
Compounds of Formula I STR1 wherein, R1 through R7 are described herein. These compounds inhibit the production of arachidonic acid products associated with 5-lipoxygenase and cyclooxygenase and are useful in the treatment of inflamm