[EN] APOPTOSIS INHIBITORS<br/>[FR] INHIBITEURS DE L'APOPTOSE
申请人:NAT INSTITUTE OF BIOLOGICAL SCIENCES BEIJING
公开号:WO2018014802A1
公开(公告)日:2018-01-25
The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition.
Pyrtriazoles, a Novel Class of Store-Operated Calcium Entry Modulators: Discovery, Biological Profiling, and in Vivo Proof-of-Concept Efficacy in Acute Pancreatitis
作者:Beatrice Riva、Alessia Griglio、Marta Serafini、Celia Cordero-Sanchez、Silvio Aprile、Rosanna Di Paola、Enrico Gugliandolo、Dalia Alansary、Isabella Biocotino、Dmitry Lim、Giorgio Grosa、Ubaldina Galli、Barbara Niemeyer、Giovanni Sorba、Pier Luigi Canonico、Salvatore Cuzzocrea、Armando A. Genazzani、Tracey Pirali
DOI:10.1021/acs.jmedchem.8b01512
日期:2018.11.8
a number of disorders, spanning from immune disorders to acute pancreatitis and have been suggested to be druggable targets. In the present contribution, we exploited the click chemistry approach to synthesize a class of SOCE modulators where the arylamide substructure that characterizes most inhibitors so far described is substituted by a 1,4-disubstituted 1,2,3-triazole ring. Within this series, inhibitors
5-Di(hetero)arylfurans are readilyaccessible in a pseudo five-component reactionvia a Sonogashira-Glaser coupling sequence followed by a superbase-mediated (KOH/DMSO) cyclization in a consecutive one-pot fashion. Besides the straightforward synthesis of natural products and biologically active molecules all representatives are particularly interesting due to their bright blue luminescence with remarkably
Pin-point chemical modification of RNA with diverse molecules through the functionality transfer reaction and the copper-catalyzed azide–alkyne cycloaddition reaction
The internal modification of RNA has been successfully achieved by the functionality transfer reaction (FTR) and following click chemistry with diverse azide compounds. The benefits of the FTR have been demonstrated by its specificity, rapidity, broad applicability, and procedure simplicity.