210686-21-8Relevant articles and documents
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: Design, synthesis, and biological evaluation
Taliani, Sabrina,Simorini, Francesca,Sergianni, Valentina,La Motta, Concettina,Da Settimo, Federico,Cosimelli, Barbara,Abignente, Enrico,Greco, Giovanni,Novellino, Ettore,Rossi, Leonardo,Gremigni, Vittorio,Spinetti, Francesca,Chelli, Beatrice,Martini, Claudia
, p. 404 - 407 (2007)
Fluorescent ligands for the peripheral-type benzodiazepine receptor (PBR) featuring the 7-nitrobenz-2-oxa-1,3-diazol-4-yl moiety were synthesized, based on N,N-dialkyl-2-phenylindol-3-ylglyoxylamides, a potent, selective class of PBR ligands previously de
Sensitive Method for the Identification of Potential Sensitizing Impurities in Reaction Mixtures by Fluorescent Nitrobenzoxadiazole-Labeled Glutathione
Tokunaga, Takashi,Yamamoto, Gaku,Takahashi, Teruki,Mukumoto, Makiko,Sato, Masayuki,Okamoto, Masahiko
, p. 3001 - 3009 (2020)
Allergic contact dermatitis is a critical issue in the development of new chemicals. Minor impurities with strong skin-sensitizing properties can be generated as byproducts. However, it is very difficult to identify these skin sensitizers in product mixtures. In this study, fluorescent nitrobenzoxadiazole-labeled glutathione (NBD-GSH) was synthesized to identify small amounts of skin sensitizers in reaction mixtures. Twelve known skin sensitizers and three nonsensitizers were reacted with NBD-GSH. Adducts formed only with the skin sensitizers, which allowed for their detection by a fluorescence detector. Liquid chromatography-mass spectrometry (LC-MS) analyses showed that NBD-GSH reacted with the skin sensitizers via its thiol and amino groups. An adduct of NBD-GSH with the strong skin sensitizer 1-chloro-2,4-dinitrobenzene was detected with a limit of detection of 6 × 10-8 mol/L by high-performance liquid chromatography with fluorescence detection. When a reaction mixture from primary alcohol oxidation was incubated with NBD-GSH, a NBD-GSH adduct formed with skin-sensitizing aldehyde impurities and could be specifically detected by LC-MS with fluorescence detection. This method will be useful for detection and identification of small amounts of skin sensitizers in raw materials, intermediates, reaction mixtures, and end products in the chemical industry.
Development and Characterization of a Fluorescent Probe for GLS1 and the Application for High-Throughput Screening of Allosteric Inhibitors
Xu, Xi,Kuang, Zijian,Han, Jie,Meng, Ying,Li, Lei,Luan, Hongyu,Xu, Pengfei,Wang, Jubo,Luo, Cheng,Ding, Hong,Li, Zhiyu,Bian, Jinlei
, p. 9642 - 9657 (2019/11/11)
Glutaminase (GLS1) is a cancer energy metabolism protein which plays a predominant role in cell growth and proliferation. Because of its major involvement in malignant tumor, small-molecule GLS1 inhibitors are urgently needed to assess its therapeutic potential and for probing their underlying biology function. Recent studies showed that targeting the allosteric binding site represented a promising strategy for identifying potent and selective GLS1 inhibitors. Herein, we present the synthesis of two fluorescent probes targeting the allosteric binding site of GLS1 and their usage as mechanistic tools in multiple applicable assay platform. The fluorescence polarization (FP)-based binding assay enables easy, fast, and reliable screen of allosteric inhibitors from our in-house compound library obtained through click chemistry method. The obtained compound C147 (named as CPU-L1) has been proved to be more potent and with greater solubility than the control compound CB839, which could serve as promising leads for further optimization as novel GLS1 inhibitors.
EASILY DECOMPOSABLE LIGNIN GENERATOR
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, (2018/02/22)
PROBLEM TO BE SOLVED: To provide an easily decomposable lignin generator containing a compound that can be introduced to a structure of lignin and can make lignin easily decomposable. SOLUTION: The easily decomposable lignin generator contains a compound represented by general formula (1), where R1 to R3 are identical or different and each represent a hydrogen atom, alkoxy group or alkyl group, R4 represents an organic group, and n represents an integer from 0 to 3. SELECTED DRAWING: None COPYRIGHT: (C)2018,JPO&INPIT
