735262-46-1Relevant academic research and scientific papers
Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety
Lv, Kai,Tao, Zeyu,Liu, Qian,Yang, Lu,Wang, Bin,Wu, Shuo,Wang, Apeng,Huang, Menghao,Liu, Mingliang,Lu, Yu
, p. 1 - 8 (2018/04/02)
We herein report the design and synthesis of benzothiazinones containing a piperidine moiety as new antitubercular agents based on the structure feature of IMB-ZR-1 discovered in our lab. Some of them were found to have good in vitro activity (MIC 1 μg/
A novel Fer/FerT targeting compound selectively evokes metabolic stress and necrotic death in malignant cells
Elkis, Yoav,Cohen, Moshe,Yaffe, Etai,Satmary-Tusk, Shirly,Feldman, Tal,Hikri, Elad,Nyska, Abraham,Feiglin, Ariel,Ofran, Yanay,Shpungin, Sally,Nir, Uri
, (2017/10/25)
Disruption of the reprogrammed energy management system of malignant cells is a prioritized goal of targeted cancer therapy. Two regulators of this system are the Fer kinase, and its cancer cell specific variant, FerT, both residing in subcellular compartments including the mitochondrial electron transport chain. Here, we show that a newly developed inhibitor of Fer and FerT, E260, selectively evokes metabolic stress in cancer cells by imposing mitochondrial dysfunction and deformation, and onset of energy-consuming autophagy which decreases the cellular ATP level. Notably, Fer was also found to associate with PARP-1 and E260 disrupted this association thereby leading to PARP-1 activation. The cooperative intervention with these metabolic pathways leads to energy crisis and necrotic death in malignant, but not in normal human cells, and to the suppression of tumors growth in vivo. Thus, E260 is a new anti-cancer agent which imposes metabolic stress and cellular death in cancer cells.
6-PHENYL-2-[((PIPERIDIN-4-YLMETHYL)-PIPERAZIN-1YL) OR PIPERAZIN 1-YLMETHYL)-PIPERIDIN-1-YL)]-IMIDAZO[2,1-B][1,3,4]THIADIAZOLE DERIVATIVES AND THEIR USE
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Page/Page column 17, (2010/09/17)
The present invention is directed to novel heterocyclic compounds, their synthesis and pharmaceutical compositions comprising them for the treatment of disorders, in particular, cancer.
Benzenesulphonamide derivatives, method for production and use thereof for treatment of pain
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Page/Page column 15, (2008/06/13)
The present invention concerns novel benzenesulphonamide compounds, defined by formula I and the description, their method of preparation and their use in therapy.
