2538-68-3Relevant 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.
Dual phenazine gene clusters enable diversification during biosynthesis
Shi, Yi-Ming,Brachmann, Alexander O.,Westphalen, Margaretha A.,Neubacher, Nick,Tobias, Nicholas J.,Bode, Helge B.
, p. 331 - 339 (2019/04/17)
Biosynthetic gene clusters (BGCs) bridging genotype and phenotype continuously evolve through gene mutations and recombinations to generate chemical diversity. Phenazine BGCs are widespread in bacteria, and the biosynthetic mechanisms of the formation of the phenazine structural core have been illuminated in the last decade. However, little is known about the complex phenazine core-modification machinery. Here, we report the diversity-oriented modifications of the phenazine core through two distinct BGCs in the entomopathogenic bacterium Xenorhabdus szentirmaii, which lives in symbiosis with nematodes. A previously unidentified aldehyde intermediate, which can be modified by multiple enzymatic and non-enzymatic reactions, is a common intermediate bridging the pathways encoded by these BGCs. Evaluation of the antibiotic activity of the resulting phenazine derivatives suggests a highly effective strategy to convert Gram-positive specific phenazines into broad-spectrum antibiotics, which might help the bacteria–nematode complex to maintain its special environmental niche.
Phenazine compound containing oxazole ring and application of phenazine compound as agricultural fungicide (by machine translation)
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, (2019/12/25)
The present invention relates to an oxazole ring-containing phenazine compound, the use of, and such a compound as an. agricultural fungicide, wherein the compound has: the following general formula (I). A compound represented R by the, formula, #, #, STR7, #, #, wherein, R represents a, 1 - 6 hydrogen, and atom, 2-4 a R halogeno-methyl group, an amino group, a phenyl group, a methoxy group, and a phenyl group. (by machine translation)
