- miRNA biosynthesis inhibitor
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The invention provides a compound shown as a formula I, or a conformational isomer thereof, or an optical isomer thereof, or a pharmaceutically acceptable salt thereof. The compound can be tightly combined with related binding proteins in an miRNA biosynthesis process and can effectively inhibit the synthesis of miRNA-21. The prepared active compound provided by the invention can be used as an miRNA-21 inhibitor, and further as a potential drug for treating malignant tumors. The formula I is shown in the description.
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Paragraph 0118; 0119; 0234-0236
(2019/06/12)
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- A Highly Efficient Heterogeneous Copper-Catalyzed Oxidative Cyclization of Benzylamines and 1,3-Dicarbonyl Compounds to Give Trisubstituted Oxazoles
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The heterogeneous copper-catalyzed cascade oxidative cyclization between benzylamines and 1,3-dicarbonyl compounds was achieved by using the 3-(2-aminoethylamino)propyl-functionalized MCM-41-immobilized copper(II) complex [MCM-41-2N-Cu(OAc) 2 ] as catalyst and t -BuOOH (TBHP) as oxidant, with iodine as additive, under mild conditions, yielding a wide variety of 2,4,5-trisubstituted oxazoles in mostly good to excellent yields. This heterogeneous copper catalyst can be facilely prepared via a simple two-step procedure from readily available and inexpensive reagents and exhibits a slightly higher activity than Cu(OAc) 2. MCM-41-2N-Cu(OAc) 2 is also easy to recover and can be recycled up to eight times with almost consistent activity. The reaction is the first example of heterogeneous copper-catalyzed intermolecular cyclization for the construction of polysubstituted oxazoles.
- Cai, Mingzhong,Tuo, Yuxin,Wei, Li,You, Shengyong
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p. 3091 - 3100
(2019/08/07)
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- Convenient route to trisubstituted oxazoles via a copper-catalysed tandem oxidative cyclisation by oxygen oxidation
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A novel copper-catalysed oxidative cyclisation has been developed for the synthesis of trisubstituted oxazoles, which is thought to proceed through cascade formation of C-N and C-O bonds by oxygen oxidation. The desired products can be obtained from readily available starting materials while avoiding hazardous materials. Therefore, a green synthetic method for the preparation of oxazoles has been found.
- Chen, Chengqun,Chen, Wenfu,Bao, Qianhong
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- Electrochemically promoted synthesis of polysubstituted oxazoles from β-diketone derivatives and benzylamines under mild conditions
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An efficient electrochemical synthesis of poly-substituted oxazoles from readily available β-diketone derivatives and benzylamines is described. This electrochemical procedure does not need hazardous oxidants and transition metal catalysts as well as molecular I2 additives. Compared with the traditional thermo-chemical method, the present electrochemical method is greener and more efficient. The Royal Society of Chemistry 2014.
- Yuan, Gaoqing,Zhu, Zechen,Gao, Xiaofang,Jiang, Huanfeng
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p. 24300 - 24303
(2014/06/24)
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- Metal-free, organocatalytic cascade formation of C-N and C-O bonds through dual sp3 C-H activation: Oxidative synthesis of oxazole derivatives
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An organocatalytic cascade reaction that involves the formation of C-N, C-O and CN bonds in one process via dual sp3 C-H activation has been developed. This protocol affords a facile metal-free methodology for the synthesis of oxazole derivatives in air under mild conditions.
- Xie, Jin,Jiang, Honglai,Cheng, Yixiang,Zhu, Chengjian
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supporting information; experimental part
p. 979 - 981
(2012/02/04)
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- Facile synthesis of polysubstituted oxazoles via A copper-catalyzed tandem oxidative cyclization
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A highly efficient synthesis of polysubstituted oxazoles was developed via a copper-catalyzed tandem oxidative cyclization. The desired products can be obtained from readily available starting materials under mild conditions. This is an attractive alterna
- Wan, Changfeng,Zhang, Jintang,Wang, Sujing,Fan, Jinmin,Wang, Zhiyong
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supporting information; experimental part
p. 2338 - 2341
(2010/08/04)
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- (2-Aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines as NHE-1 inhibitors
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A series of (2-aryl-5-methylimidazol-4-ylcarbonyl)guanidines and (2-aryl-5-methyloxazol-4-ylcarbonyl)guanidines were synthesized and evaluated as NHE-1 inhibitors. The structure-activity relationships well matched those of furan derivatives, which were previously investigated. The (2,5-disubstituted)phenyl compounds showed better activities than the other analogues in both imidazole and oxazole compounds. Especially, 2-(2,5-dichlorophenyl)imidazole 52, and 2-(2-methoxy-5-chlorophenyl)imidazole 54 compounds exhibited potent cardioprotective efficacy both in vitro and in vivo as well as high NHE-1 inhibitory activities.
- Lee, Sunkyung,Yi, Kyu Yang,Youn, Sung Jun,Lee, Byung Ho,Yoo, Sung-eun
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scheme or table
p. 1329 - 1331
(2009/10/02)
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