130190-35-1Relevant articles and documents
Identification of Pyruvate Carboxylase as the Cellular Target of Natural Bibenzyls with Potent Anticancer Activity against Hepatocellular Carcinoma via Metabolic Reprogramming
Chen, Yuwen,Huang, Yulan,Jiao, Wei,Li, Fu,Li, Suiyan,Li, Wenhua,Lin, Yuan,Liu, Wanli,Ma, Yuling,Sheng, Yuwen,Suksamrarn, Apichart,Wang, Fei,Wang, Jing,Wei, Xiao,Wisanwattana, Wisanee,Wu, Wenbi,Zeng, Zhongqiu,Zhang, Guolin,Zhang, Jichao,Zhu, Qiyu
, (2022/01/03)
Cancer cell proliferation in some organs often depends on conversion of pyruvate to oxaloacetate via pyruvate carboxylase (PC) for replenishing the tricarboxylic acid cycle to support biomass production. In this study, PC was identified as the cellular target of erianin using the photoaffinity labeling-click chemistry-based probe strategy. Erianin potently inhibited the enzymatic activity of PC, which mediated the anticancer effect of erianin in human hepatocellular carcinoma (HCC). Erianin modulated cancer-related gene expression and induced changes in metabolic intermediates. Moreover, erianin promotes mitochondrial oxidative stress and inhibits glycolysis, leading to insufficient energy required for cell proliferation. Analysis of 14 natural analogs of erianin showed that some compounds exhibited potent inhibitory effects on PC. These results suggest that PC is a cellular target of erianin and reveal the unrecognized function of PC in HCC tumorigenesis; erianin along with its analogs warrants further development as a novel therapeutic strategy for the treatment of HCC.
Preparation and application of 3,4-diaryl-1,2,5-oxadiazole oxide
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Paragraph 0103; 0104; 0106; 0107, (2017/08/02)
The invention belongs to the technical field of medicine, and relates to preparation and application of a 3,4-diaryl-1,2,5-oxadiazole oxide, in particular to a 3,4-diaryl-1,2,5-oxadiazole oxide compound and application thereof in preparation of anti-tumor medicine by serving as a tumor cell proliferation inhibitor. The compound is shown as the general formula I or general formula II (please see the formulas in the description), wherein R1-R5 are described as the claims and the description.
Synthesis and biological evaluation of novel 3,4-diaryl-1,2,5-selenadiazol analogues of combretastatin A-4
Guan, Qi,Yang, Fushan,Guo, Dandan,Xu, Jingwen,Jiang, Mingyang,Liu, Chunjiang,Bao, Kai,Wu, Yingliang,Zhang, Weige
, p. 1 - 9 (2015/02/05)
A set of novel selenium-containing heterocyclic analogues of combretastatin A-4 (CA-4) have been designed and synthesised using a rigid 1,2,5-selenadiazole as a linker to fix the cis-orientation of ring-A and ring-B. All of the target compounds were evalu