6287-57-6Relevant academic research and scientific papers
MLKL INHIBITORS
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, (2018/09/26)
Purine derivatives that inhibit cellular necroptosis and/or human MLKL, pharmaceutical compositions thereof, and methods of treating an MLKL-mediated disorder with an effective amount of the compound or composition. Said MLKL-mediated disorder is pathology associated necroptosis, including ischemia-reperfusion damage, neurodegeneration, and inflammatory diseases such as acute pancreatitis, multiple sclerosis, inflammatory bowel disease, and allergic colitis.
Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineage kinase domain-like protein
Yan, Bo,Liu, Lei,Huang, Shaoqiang,Ren, Yan,Wang, Huayi,Yao, Zhenglin,Li, Lin,Chen, She,Wang, Xiaodong,Zhang, Zhiyuan
, p. 3637 - 3640 (2017/04/03)
We report the development of novel Mixed Lineage Kinase Domain-Like protein (MLKL) inhibitors with single nanomolar potency (compound 15 is also named as TC13172). Using the converting biochemistry to chemistry activity-based protein profiling (BTC-ABPP) method, we were able to determine that the inhibitors covalently bind to Cysteine86 (Cys-86) of MLKL. This is the first example of the use of LC-MS/MS to identify the binding site of an MLKL inhibitor. The novel MLKL inhibitors provide powerful tools to study the biological function of MLKL and demonstrate that MLKL should be viewed as a druggable target.
Antioxidant properties of thio-caffeine derivatives: Identification of the newly synthesized 8-[(pyrrolidin-1-ylcarbonothioyl)sulfanyl]caffeine as antioxidant and highly potent cytoprotective agent
Jasiewicz, Beata,Sierakowska, Arleta,Wandyszewska, Natalia,War?ajtis, Beata,Rychlewska, Urszula,Wawrzyniak, Rafa?,Mrówczyńska, Lucyna
supporting information, p. 3994 - 3998 (2016/08/01)
A series of nine thio-caffeine analogues were synthesized and characterised by NMR, FT-IR and MS spectroscopic methods. Molecular structures of four of them were determined using single crystal X-ray diffraction methods. The antioxidant properties of all
Copper-catalyzed direct thiolation of xanthines and related heterocycles with disulfides
He, Zuying,Luo, Fang,Li, Yinglong,Zhu, Gangguo
supporting information, p. 5907 - 5910 (2013/10/21)
A novel copper-catalyzed, base-free direct thiolation of xanthines and related heterocycles is described, featuring the use of inexpensive Cu(OAc) 2·H2O as the catalyst, O2 as a clean and cheap oxidant, and easy-to-handle
