105485-74-3Relevant academic research and scientific papers
Identification of Pyruvate Carboxylase as the Cellular Target of Natural Bibenzyls with Potent Anticancer Activity against Hepatocellular Carcinoma via Metabolic Reprogramming
Sheng, Yuwen,Chen, Yuwen,Zeng, Zhongqiu,Wu, Wenbi,Wang, Jing,Ma, Yuling,Lin, Yuan,Zhang, Jichao,Huang, Yulan,Li, Wenhua,Zhu, Qiyu,Wei, Xiao,Li, Suiyan,Wisanwattana, Wisanee,Li, Fu,Liu, Wanli,Suksamrarn, Apichart,Zhang, Guolin,Jiao, Wei,Wang, Fei
, p. 460 - 484 (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.
Design, synthesis and biological evaluation of 3,4-diaryl-1,2,5-oxadiazole-2/5-oxides as highly potent inhibitors of tubulin polymerization
Hong, Yilang,Zhao, Yinglin,Yang, Lei,Gao, Minghuan,Li, Long,Man, Shuai,Wang, Zhan,Guan, Qi,Bao, Kai,Zuo, Daiying,Wu, Yingliang,Zhang, Weige
, p. 287 - 296 (2019/06/14)
Structure-activity relationships for rigid analogues of combretastatin A-4 (CA-4) were investigated, leading to the discovery of a series of 3,4-diaryl-1,2,5-oxadiazole-N-oxides. Among them, 7n′ and 7n′′ showed remarkable antiproliferative activities agai
Fluoro-substitution diphenylethane derivative and preparation method and application thereof
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Paragraph 0042; 0055-0057; 0062-0065, (2019/12/25)
The invention relates to a fluoro-substitution diphenylethane derivative. The fluoro-substitution diphenylethane derivative is characterized in that the structure of the fluoro-substitution diphenylethane derivative is shown as the general formula (I) (pl
Synthesis and biological evaluation of 2,3-diarylthiophene analogues of combretastatin A-4
Wang, Zhan,Yang, Qingkun,Bai, Zhaoshi,Sun, Jun,Jiang, Xuewei,Song, Hongrui,Wu, Yingliang,Zhang, Weige
supporting information, p. 971 - 976 (2015/05/27)
A series of novel 2,3-diarylthiophene analogues of combretastatin A-4 (CA-4) were designed with a rigid thiophene moiety to retain the cis-olefin configuration of CA-4 and were subsequently synthesised. All of the target compounds were evaluated for their
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
Synthesis and cytotoxic activities of 4,5-diarylisoxazoles
Sun, Chang-Ming,Lin, Lee-Gin,Yu, Hsi-Jung,Cheng, Chih-Yu,Tsai, Ya-Chuan,Chu, Chi-Wei,Din, Yi-Hui,Chau, Yat-Pang,Don, Ming-Jaw
, p. 1078 - 1081 (2007/10/03)
A series of 4,5-diarylisoxazoles related to combretastatin A-4 (CA-4) were synthesized and evaluated for cytotoxicity against three human cancer cell lines. Among them, compound 6e showed better cytotoxic activity than CA-4 in HeLa and HepG2 cell lines as
REGIOSPECIFICALLY SUBSTITUTED DEOXIBENZOINS BY HORNER CONDENSATION OF AROMATIC ALDEHYDES WITH O-PROTECTED α-ARYL-α-HYDROXYMETHANEPHOSPHONATES
Napolitano, Elio,Ramacciotti, Antonella
, p. 19 - 22 (2007/10/02)
Dimethyl-α-aryl-α-hydroxymethanephosphonates, prepared by addition of dimethyl phosphite to the appropriate aromatic aldehyde, Ar-CHO, have been protected at oxygen by reaction with 3,4-dihydro-2H-pyran catalyzed by p-toluenesulphonic acid and condensed w
A Simple Synthesis of (+/-)-Combretastatin
Latey, P. P.,Deshpande, V. H.
, p. 299 - 300 (2007/10/02)
A simple synthesis of (+/-)-combretastatin (1) has been described starting from 3,4,5-trimethoxybenzaldehyde and isovanillin.
