715-12-8Relevant academic research and scientific papers
Styrene sulfone NLRP3 inflammasome inhibitor, preparation method and application thereof
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Paragraph 0053; 0078-0081; 0082-0083, (2020/10/30)
The invention relates to the field of styrene sulfone compounds and NLRP3 inhibitors, and particularly provides a styrene sulfone NLRP3 inflammasome inhibitor, a preparation method and application thereof, wherein the inhibitor is represented by a formula (1), n is selected from 0 and 1, X is selected from N and O, R1 is selected from different electron withdrawing or electron donating substituents, and R2 is selected from different fat or aromatic substituents. According to the invention, it is verified that the compounds represented by the general formula have NLRP3 inhibitory activity.
Metal-Free Route to Carboxylated 1,4-Disubstituted 1,2,3-Triazoles from Methoxycarbonyl-Modified Vinyl Sulfone
Das, Jayanta,Dey, Santu,Pathak, Tanmaya
, (2019/11/29)
A metal-free alternative to the regioselective synthesis of carboxylated 1,4-disubstituted 1,2,3-triazoles (1,4-cDTs) has been accomplished. A methoxycarbonyl-substituted vinyl sulfone on reactions with organic azides resulted in the formation of 1,4-cDTs
Design and Synthesis of Novel 4-Phenoxyquinolines Bearing 3-Hydrosulfonylacrylamido or 1H-Imidazole-4-carboxamido Scaffolds as c-Met Kinase Inhibitors
Wang, Jiao,Xie, Lijun,Wang, Yu,Wang, Xiaoqiang,Xi, Shuancheng,Zeng, Tianfang,Gong, Ping,Zhai, Xin
, (2017/02/15)
A series of novel 6,7-disubstituted-4-phenoxyquinoline derivatives bearing (E)-3-hydrosulfonylacrylamido or 1H-imidazole-4-carboxamido moieties were designed, synthesized and evaluated for their cytotoxicity against A549, MKN-45, and HT-29 cancer cell lines in vitro. All the target compounds showed moderate to significant cytotoxic activity against the tested cells with IC50 values ranging from 0.13 to 2.65 μM. Five of them were further examined for their inhibitory activity against c-Met kinase, which identified compound 30 as a promising agent (c-Met IC50 = 1.52 nM) with IC50 values of 0.24, 0.45, and 0.13 μM against HT-29, MKN-45, and A549 cells, respectively.
Design, synthesis and biological evaluation of novel 4-(2-fluorophenoxy)quinoline derivatives as selective c-Met inhibitors
Wang, Xiaoqiang,Jiang, Nan,Zhao, Sijia,Xi, Shuancheng,Wang, Jiao,Jing, Tongfei,Zhang, Wenyu,Guo, Ming,Gong, Ping,Zhai, Xin
, p. 886 - 896 (2017/02/05)
Two novel series of 6,7-disubstituted-4-(2-fluorophenoxy)quinoline derivatives bearing 1H-imidazole-4-carboxamido or (E)-3-hydrosulfonylacrylamido motifs (16–31 and 32–42) were designed, synthesized and evaluated for their in vitro cytotoxic activity. Most of the compounds exhibited moderate to excellent potency against tested three cell lines, and fifteen compounds were further examined for their inhibitory activity against c-Met kinase. The most promising compound 16 (c-Met kinase [IC50]?=?1.1?nM) demonstrated high selectivity and remarkable cytotoxicity against HT-29, MKN-45 and A549 cells with IC50values of 0.08, 0.22 and 0.07?μM, which were 3.1-, 1.4- and 2.1-fold more active than Foretinib. The preliminary structure-activity relationships as well as molecular docking disclosed that 1H-imidazole-4-carboxamido as a linker was of great importance for the antitumor activity.
Transition-metal-free synthesis of (E)-vinyl sulfones from vinyl halides in water
Liang, Shuai,Zhang, Ruo-Yi,Wang, Gao,Chen, Shan-Yong,Yu, Xiao-Qi
supporting information, p. 7050 - 7053 (2013/11/06)
A practical transition-metal-free procedure for the synthesis of (E)-vinyl sulfones through the coupling of vinyl halides with sodium sulfinates in water is reported. The reaction is strongly influenced by the presence of acids, and the use of nBu4NBr promotes its efficiency. A metal-free procedure for the synthesis of vinyl sulfones through the coupling of vinyl halides with sodium sulfinates in water is presented. The reaction is strongly influenced by the presence of acids, and the use of nBu4NBr promotes its efficiency. Copyright
Regio- and Stereo-selective Synthesis of β-Sulphonyl-α,β-Unsaturated Carbonyl Compounds via an Iodosulphonylation-Dehydroiodination Raction
Najera, Carmen,Baldo, Beatriz,Yus, Miguel
, p. 1029 - 1032 (2007/10/02)
α,β-Unsaturated carbonyl compounds underwent regiospecific iodosulphonylation with toluene-p-sulphonyl iodide or sodium toluene-p-sulphinate and iodine to afford products (2), which were stereoselectively dehydroiodinated by triethylamine to give β-sulphonyl derivatives (3).The reactivity of compounds (3) as cationic β-acylvinyl equivalents, tested with amines or thiophenol, gave compounds (4) resulting from a displacement reaction.
