《Design, Synthesis, and Biological Activity of 1,2,3-Triazolobenzodiazepine BET Bromodomain Inhibitors》 was written by Sharp, Phillip P.; Garnier, Jean-Marc; Hatfaludi, Tamas; Xu, Zhen; Segal, David; Jarman, Kate E.; Jousset, Helene; Garnham, Alexandra; Feutrill, John T.; Cuzzupe, Anthony; Hall, Peter; Taylor, Scott; Walkley, Carl R.; Tyler, Dean; Dawson, Mark A.; Czabotar, Peter; Wilks, Andrew F.; Glaser, Stefan; Huang, David C. S.; Burns, Christopher J.. Recommanded Product: 844501-71-9This research focused ontriazolo benzo diazepine preparation BET domain inhibitor anticancer agent. The article conveys some information:
A number of diazepines are known to inhibit bromo- and extra-terminal domain (BET) proteins. Their BET inhibitory activity derives from the fusion of an acetyl-lysine mimetic heterocycle onto the diazepine framework. Herein we describe a straightforward, modular synthesis of novel 1,2,3-triazolobenzodiazepines and show that the 1,2,3-triazole acts as an effective acetyl-lysine mimetic heterocycle. Structure-based optimization of this series of compounds led to the development of potent BET bromodomain inhibitors, e.g., I, with excellent activity against AF9-MLL-driven leukemic cells, concomitant with a reduction in c-MYC expression. These novel benzodiazepines therefore represent a promising class of therapeutic BET inhibitors.3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9Recommanded Product: 844501-71-9) was used in this study.
3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole(cas: 844501-71-9) belongs to pyrazoles. Pyrazoles are commonly used scaffold molecules in drug discovery projects. The use of pyrazole derivatives is based on their analgesic, neuroleptic, anticonvulsant, monoamine oxidase inhibitory, anti-inflammatory, antipyretic, antiarrhythmic, sedative, muscle relaxant, antidiabetic and antibacterial activities. Recommanded Product: 844501-71-9
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Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics