347320-93-8Relevant academic research and scientific papers
Chemoselective regulation of TREK2 channel: Activation by sulfonate chalcones and inhibition by sulfonamide chalcones
Kim, Eun-Jin,Ryu, Hyung Won,Curtis-Long, Marcus J.,Han, Jaehee,Kim, Jun Young,Cho, Jung Keun,Kang, Dawon,Park, Ki Hun
, p. 4237 - 4239 (2010)
Although it has not been extensively studied, a significant volume of literature suggests that TREK2 will probably turn out to be an important channel in charge of tuning neuronal transmitter and hormone levels. Thus, pharmacological tools which can manip
Purine-ring-containing benzene sulfonamide chalcone derivative and preparation and application methods thereof
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Paragraph 0049, (2019/01/05)
The invention discloses a purine-ring-containing benzene sulfonamide chalcone derivative and preparation and application methods thereof. The purine-ring-containing benzene sulfonamide chalcone derivative has a formula (I) shown as below, in which R1 is 4-oxymethyl, 4-tert-butyl, 4-methyl, 4-flouride, 4-bromide, 2-methyl, 2-fluoride, 2-chloride, 2-bromide and hydrogen atom and R2 is methyl, ethyland benzyl. The purine-ring-containing benzene sulfonamide chalcone derivative can inhibit tobacco mosaic virus, cucumber mosaic virus, potato Y virus and southern rice black-streaked dwarf virus.
Discovery and structure-activity relationship of novel 4-hydroxy-thiazolidine-2-thione derivatives as tumor cell specific pyruvate kinase M2 activators
Li, Ridong,Ning, Xianling,Zhou, Shuo,Lin, Zhiqiang,Wu, Xingyu,Chen, Hong,Bai, Xinyu,Wang, Xin,Ge, Zemei,Li, Runtao,Yin, Yuxin
, p. 48 - 65 (2017/11/23)
Pyruvate kinase M2 isoform (PKM2) is a crucial protein responsible for aerobic glycolysis of cancer cells. Activation of PKM2 may alter aberrant metabolism in cancer cells. In this study, we discovered a 4-hydroxy-thiazolidine-2-thione compound 2 as a novel PKM2 activator from a random screening of an in-house compound library. Then a series of novel 4-hydroxy-thiazolidine-2-thione derivatives were designed and synthesized for screening as potent PKM2 activators. Among these, some compounds showed higher PKM2 activation activity than lead compound 2 and also exhibited significant anti-proliferative activities on human cancer cell lines at nanomolar concentration. The compound 5w was identified as the most potent antitumor agent, which showed excellent anti-proliferative effects with IC50 values from 0.46 μM to 0.81 μM against H1299, HCT116, Hela and PC3 cell lines. 5w also showed less cytotoxicity in non-tumor cell line HELF compared with cancer cells. In addition, Preliminary pharmacological studies revealed that 5w arrests the cell cycle at the G2/M phase in HCT116 cell line. The best PKM2 activation by compound 5t was rationalized through docking studies.
Novel 5-Hydroxy, 5-Substituted Benzenesulfonamide Pyrimidine-2,4,6-Triones Attenuate Lipopolysaccharide-Induced Acute Lung Injury via Inhibition of the Gelatinases, MMP-2 and MMP-9
He, Wei,Jiang, Jie,Yu, Ze-Qian,Zhou, Jia-Hua
, p. 251 - 257 (2016/08/26)
(Table presented.). A novel series of ten 5-hydroxy, 5-substituted benzene sulfonamide pyrimidine-2,4,6-triones were synthesized and their structures ascertained using 1H-NMR, 13C-NMR, mass and elemental analysis. These compounds wer
Inhibitory evaluation of sulfonamide chalcones on β-secretase and acylcholinesterase
Kang, Jae Eun,Cho, Jung Keun,Curtis-Long, Marcus J.,Ryu, Hyung Won,Kim, Jin Hyo,Kim, Hye Jin,Yuk, Heung Joo,Kim, Dae Wook,Park, Ki Hun
, p. 140 - 153 (2013/04/23)
The action of β-secretase (BACE1) is strongly correlated with the onset of Alzheimer's disease (AD). Aminochalcone derivatives were examined for their ability to inhibit BACE1. Parent aminochalcones showed two digit micromolar IC50s against BACE1. Potency
Pyrazolines for the Modulation of PKM2
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Page/Page column 91, (2012/12/13)
The invention relates to pyrazoline substituted compounds and methods for activating PKM2. The compounds and methods are useful in treating or preventing a disease or disorder selected from cancer, cell proliferative disorder, inflammatory disorder, metabolic disorder, and immune system disorder.
Evaluation of anti-pigmentary effect of synthetic sulfonylamino chalcone
Seo, Woo Duck,Ryu, Young Bae,Curtis-Long, Marcus J.,Lee, Chan Woo,Ryu, Hyung Won,Jang, Ki Chang,Park, Ki Hun
scheme or table, p. 2010 - 2017 (2010/07/04)
The 4′-(p-toluenesulfonylamino)-4-hydroxychalcone (TSAHC), which bears inhibitory chemotypes for both α-glucosidase and tyrosinase, was evaluated for tyrosinase activity and depigmenting ability relative to compounds designed to only target tyrosianse act
α-Mercaptoketone based histone deacetylase inhibitors
Wash, Paul L.,Hoffman, Timothy Z.,Wiley, Brandon M.,Bonnefous, Celine,Smith, Nicholas D.,Sertic, Michael S.,Lawrence, Charles M.,Symons, Kent T.,Nguyen, Phan-Manh,Lustig, Kevin D.,Guo, Xin,Annable, Tami,Noble, Stewart A.,Hager, Jeffrey H.,Hassig, Christian A.,Malecha, James W.
scheme or table, p. 6482 - 6485 (2009/10/01)
In an effort to discover novel non-hydroxamic acid histone deacetylase (HDAC) inhibitors, a novel α-mercaptoketone was identified in a high-throughput screen. Lead optimization of the screening hit, led to a number of potent HDAC inhibitors. In particular, α-mercaptoketone 19y (KD5150) exhibited nanomolar in vitro activity and inhibition of tumor growth in vivo.
