3752-25-8Relevant articles and documents
Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia
Zhang, Peng,Min, Zhihui,Gao, Yang,Bian, Jiang,Lin, Xin,He, Jie,Ye, Deyong,Li, Yilin,Peng, Chao,Cheng, Yunfeng,Chu, Yong
, p. 7341 - 7358 (2021/06/28)
Recently, irreversible inhibitors have attracted great interest in antitumors due to their advantages of forming covalent bonds to target proteins. Herein, some benzothiazepinone compounds (BTZs) have been designed and synthesized as novel covalent GSK-3β inhibitors with high selectivity for the kinase panel. The irreversible covalent binding mode was identified by kinetics and mass spectrometry, and the main labeled residue was confirmed to be the unique Cys14 that exists only in GSK-3β. The candidate 4-3 (IC50 = 6.6 μM) showed good proliferation inhibition and apoptosis-inducing ability to leukemia cell lines, low cytotoxicity on normal cell lines, and no hERG inhibition, which hinted the potential efficacy and safety. Furthermore, 4-3 exhibited decent pharmacokinetic properties in vivo and remarkably inhibited tumor growth in the acute promyelocytic leukemia (APL) mouse model. All the results suggest that these newly irreversible BTZ compounds might be useful in the treatment of cancer such as APL.
Dual Nickel/Ruthenium Strategy for Photoinduced Decarboxylative Cross-Coupling of α,β-Unsaturated Carboxylic Acids with Cycloketone Oxime Esters
Gao, Ang,Jiang, Run-Chuang,Liu, Chuang-Chuang,Liu, Qi-Le,Lu, Xiao-Yu,Xia, Ze-Jie
supporting information, p. 8829 - 8842 (2021/06/30)
Herein, a dual nickel/ruthenium strategy is developed for photoinduced decarboxylative cross-coupling between α,β-unsaturated carboxylic acids and cycloketone oxime esters. The reaction mechanism is distinct from previous photoinduced decarboxylation of α,β-unsaturated carboxylic acids. This reaction might proceed through a nickelacyclopropane intermediate. The C(sp2)-C(sp3) bond constructed by the aforementioned reaction provides an efficient approach to obtaining various cyanoalkyl alkenes, which are synthetically valuable organic skeletons in organic and medicinal chemistry, under mild reaction conditions. The protocol tolerates many critical functional groups and provides a route for the modification of complex organic molecules.
A novel Co(II) based multifunctional metal-organic framework: Synthesis, fluorescence sensing and magnetic analysis
Sun, Han-yang,Wang, Zi-run,Li, Xue,Han, Shuang,Wang, Jia-jun,Li, Wen-fang,Liu, Chun-ling,Li, Chuan-bi
, p. 750 - 756 (2018/12/11)
A new coordination Co(II) complex, namely, [Co2(DIPT)4(PClA)2Cl2]·H2O (NCl-1) (DIPT = 2-(2,4-dichlorophenyl) -1H-imidazo [4,5–f]-[1,10]phenanthroline, HPClA = 3-(2-chlorophenyl)acrylie) has been synthesized under solvothermal conditions and structurally characterized by elemental analysis, IR spectroscopy, single-crystal X-ray diffraction analysis, nitrogen adsorption analysis and powder X-ray diffraction. NCl-1 constructed by six coordinated mode with metal center and connected different ligands and ions, exhibits a three-dimensional structure under interactions of hydrogen bond and π-π stacking interactions. The luminescence explorations demonstrated that NCl-1 exhibits highly selective and sensitive sensing for organic solvents (MeOH) and metal ion (Fe3+). Furthermore, magnetic analysis indicated that NCl-1 also own the property of anti ferromagnetic.
