651293-08-2Relevant academic research and scientific papers
SULFONAMIDE COMPOUNDS AND THE USE THEREOF IN THE TREATMENT OF CANCER
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Paragraph 00181, (2021/04/23)
The present disclosure relates generally to a class of sulfonamide-based compounds, compositions containing the same and the therapeutic use of the compounds in the treatment of cancer.
Design, synthesis and biological evaluation of artemisinin derivatives containing fluorine atoms as anticancer agents
Li, Shu,Li, Gongming,Yang, Xiaohong,Meng, Qian,Yuan, Shuo,He, Yun,Sun, Dequn
supporting information, p. 2275 - 2278 (2018/05/24)
Ten novel artemisinin derivatives containing fluorine atoms were synthesized and their structures were confirmed by 1H NMR, 13C NMR and HRMS technologies in this study. The in vitro cytotoxicity against U87MG, SH-SY5Y, MCF-7, MDA-MB-231, A549 and A375 cancer cell lines was evaluated by MTT assay. Compound 9j was the most potent anti-proliferative agent against the human breast cancer MCF-7 cells (IC50 = 2.1 μM). The mechanism of action of compound 9j was further investigated by analysis of cell apoptosis and cell cycle. Compound 9j induced cell apoptosis and arrested cell cycle at G1 phase in MCF-7 cells. Our promising findings indicated that the compound 9j could stand as potential lead compound for further investigation.
Phenylquinoline transient receptor potential vanilloid 1 antagonists for the treatment of pain: Discovery of 1-(2-phenylquinoline-4-carbonyl)-N-(4-(trifluoromethyl)phenyl)pyrrolidine-3-carboxamide
Liao, Chen,Liu, Yan,Liu, Chunxia,Zhou, Jiaqi,Li, Huilan,Wang, Nasi,Li, Jieming,Liu, Taiyu,Ghaleb, Hesham,Huang, Wenlong,Qian, Hai
, p. 845 - 854 (2018/01/10)
Reported herein is the design, synthesis, and pharmacologic characterization of a class of TRPV1 antagonists constructed on a phenylquinoline platform that evolved from Cinchophen lead. This design composes three sections: a phenylquinoline headgroup attached to an aliphatic carboxamides, which is tethered at a phenyl tail group. Optimization of this design led to the identification of 37, comprising a pyrrolidine linker and a trifluoromethyl–phenyl tail. In the TRPV1 functional assay, using cells expressed hTRPV1, 37 antagonized capsaicin-induced Ca2+ influx, with an IC50 value of 10.2 nM. In the complete mice analgesic model, 37 exhibited better antinociceptive activity than the positive control BCTC in diverse pain models. All of these results suggested that 37 could be considered as a lead candidate for the further development of antinociceptive drugs.
Discovery libraries targeting the major enzyme classes: The serine hydrolases
Otrubova, Katerina,Srinivasan, Venkat,Boger, Dale L.
supporting information, p. 3807 - 3813 (2014/09/16)
Two libraries of modestly reactive ureas containing either electron-deficient acyl anilines or acyl pyrazoles were prepared and are reported as screening libraries for candidate serine hydrolase inhibitors. Within each library is a small but powerful subs
The design and synthesis of novel, potent and orally bioavailable N-aryl piperazine-1-carboxamide CCR2 antagonists with very high hERG selectivity
Cumming, John G.,Bower, Justin F.,Waterson, David,Faull, Alan,Poyser, Philip J.,Turner, Paul,McDermott, Benjamin,Campbell, Andrew D.,Hudson, Julian,James, Michael,Winter, Jon,Wood, Christine
scheme or table, p. 3895 - 3899 (2012/07/03)
A novel N-aryl piperazine-1-carboxamide series of human CCR2 chemokine receptor antagonists was discovered. Early analogues were potent at CCR2 but also inhibited the hERG cardiac ion channel. Structural modifications which decreased lipophilicity and basicity resulted in the identification of a sub-series with an improved margin over hERG. The pharmacological and pharmacokinetic properties of the lead compound from this series, N-(3,4-dichlorophenyl)-4-[(2R)-4-isopropylpiperazine-2-carbonyl] piperazine-1-carboxamide, are described.
