6311-37-1Relevant articles and documents
Green synthesis method of bromoaromatic amine and alpha-bromoaromatic ketone
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Paragraph 0026-0029, (2017/07/21)
The invention discloses a green synthesis method of bromoaromatic amine and alpha-bromoaromatic ketone. The synthesis method comprises: adopting hydrobromic acid as a brominating agent, adopting 2-methylpyridine nitrate as a catalyst, and adopting molecular oxygen as an oxidizing agent, brominating an aromatic compound with a structure shown in formula (1) or aromatic ketone with a structure shown in formula (2) or (3), and preparing corresponding bromoaromatic amine or alpha-bromoaromatic ketone. The synthesis method is wide in substrate application reaction, high in atom utilization rate, capable of avoiding the application of the transitional metal element and volatile organic solvent and has the characteristics of economical efficiency and environmental protection. (Shown in the description).
Measurement of long-range interatomic distances by solid-state tritium-NMR spectroscopy
Yuen, Alexander K. L.,Lafon, Olivier,Charpentier, Thibault,Roy, Myriam,Brunet, Francine,Berthault, Patrick,Sakellariou, Dimitrios,Robert, Bruno,Rimsky, Sylvie,Pillon, Florence,Cintrat, Jean-Christophe,Rousseau, Bernard
supporting information; experimental part, p. 1734 - 1735 (2010/04/25)
(Chemical Equation Presented) For the structural determination of a ligand bound to an amorphous macromolecular system, solid-state NMR can be used to provide interatomic distances. It is shown here that selective labeling in discrete locations with tritium enables accurate measurement of long-range distances owing to the high gyromagnetic ratio of this nucleus, without structural modification of the molecule. This approach gives access to the largest NMR distance ever measured between two nuclei (14.4 A). 3H MAS NMR appears to be a promising tool for structural applications in the biological and material sciences. Copyright
Non-peptidic substrate-mimetic inhibitors of Akt as potential anti-cancer agents
Kayser-Bricker, Katherine J.,Glenn, Matthew P.,Lee, Sang Hoon,Sebti, Said M.,Cheng, Jin Q.,Hamilton, Andrew D.
supporting information; experimental part, p. 1764 - 1771 (2009/09/05)
Akt has emerged as a critical target for the development of anti-cancer therapies. It has been found to be amplified, overexpressed, or constitutively activated in numerous human malignancies with oncogenesis derived from the simultaneous promotion of cell survival and suppression of apoptosis. A valuable alternative to the more common ATP-mimetic based chemotherapies is a substrate-mimetic approach, which has the potential advantage of inherent specificity of the substrate-binding pocket. In this paper we present the development of high affinity non-peptidic, substrate-mimetic inhibitors based on the minimum GSK3β substrate sequence. Optimization of initial peptidic leads resulted in the development of several classes of small molecule inhibitors, which have comparable potency to the initial peptidomimetics, while eliminating the remaining amino acid residues. We have identified the first non-peptidic substrate-mimetic lead inhibitors of Akt 29a-b, which have affinities of 17 and 12 μM, respectively. This strategy has potential to provide a useful set of molecular probes to assist in the validation of Akt as a potential target for anti-cancer drug design.
