54420-95-0Relevant articles and documents
Design, synthesis and biological evaluations of diverse Michael acceptor-based phenazine hybrid molecules as TrxR1 inhibitors
Zhong, Yucheng,Liu, Jing,Cheng, Xiangyu,Zhang, Hao,Zhang, Chunhua,Xia, Zhuolu,Wu, Zhongxi,Zhang, Lu,Zheng, Yuting,Gao, Zhanyu,Jiang, Zhidong,Wang, Zhixiang,Huang, Dechun,Lu, Yuanyuan,Jiang, Feng
, (2021/03/01)
A series of novel phenazine derivatives (1~27) containing the Michael acceptor scaffolds were designed and synthesized in this study. Some compounds exhibited selective cytotoxicity against Bel-7402 cancer cell line in vitro, in which compound 26 were found to have the best antiproliferative activity. Meanwhile, compound 26 showed no obvious cell toxicity against human normal liver epithelial L02 cells, which means this compound possessed a better safety potential. In the following research, compound 26 was verified to inhibit TrxR1 enzyme activity, ultimately resulting in cellular molecular mechanism events of apoptosis including growth of intracellular ROS level, depletion of reduced Trx1, liberation of ASK1 and up-regulation of p38, respectively. Together, all these evidences implicated that compound 26 acted as the TrxR1 inhibitor against Bel-7402 cells, and could activate apoptosis through the ROS-Trx-ASK1-p38 pathway.
Phenazine derivative serving as TrxR1 inhibitor, intermediate product, preparation methods of phenazine derivative and intermediate product and application of phenazine derivative
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Paragraph 0023; 0033-0034, (2019/09/14)
The invention discloses a phenazine derivative which has a structure shown in a general formula I and serves as a TrxR1 inhibitor, an intermediate product, and a preparation method and application ofthe phenazine derivative. In the formula I, R is H or CH3; R is selected from H, CH2N(CH3)2, phenyl, (4-fluoro)-phenyl, (3-trifluoromethyl)-phenyl, (4-chloro)-phenyl and (2,5-dichloro)-phenyl; and R is H. The phenazine derivative disclosed by the invention has significant inhibitory activity on TrxR1, especially has significant anti-proliferative activity on HepG2 cell strains, and can beused for preparing anti-tumor drugs.
Phenazine carboxylate compound and use thereof
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Paragraph 0058; 0059; 0060; 0061, (2016/10/08)
The invention discloses a phenazine carboxylate compound which is represented by a formula I shown in the description, wherein R is selected from C4-C6 alkyl, C3-C6 alkenyl, C3-C6 alkynyl, aryl C1-C3 alkyl or C3-C8 cycloalkyl; the aryl is selected from a benzene ring, a pyridine ring, a pyrimidine ring, a pyrazine ring, a pyridazine ring, a furan ring, a thiophene ring, a pyrazol ring, an imidazole ring and a triazole ring which are substituted by 1-5 same or different R1; R1 is selected from hydrogen, halogen, hydroxyl, amino, nitryl, cyano, C1-C6 alkyl, C1-C6 halogenated alkyl, C1-C6 alkyl amino, C1-C6 halogenated alkyl amino, C1-C6 alkoxyl or C1-C6 halogenated alkoxyl. The compound represented by the formula I has excellent sterilizing bacterial and can be used for preventing plant fungi diseases.
