86601-34-5Relevant articles and documents
Discovery of simplified benzazole fragments derived from the marine benzosceptrin B as necroptosis inhibitors involving the receptor interacting protein Kinase-1
Al-Mourabit, Ali,Bach, Stéphane,Baratte, Blandine,Benchekroun, Mohamed,Delehouzé, Claire,Ermolenko, Ludmila,Iorga, Bogdan I.,Josselin, Béatrice,Nedev, Hristo,Ruchaud, Sandrine,Souab, Mohamed,Tran, Minh Quan,Vagneux, Agathe
, (2020)
With the aim to develop new chemical tools based on simplified natural metabolites to help deciphering the molecular mechanism of necroptosis, simplified benzazole fragments including 2-aminobenzimidazole and the 2-aminobenzothiazole analogs were prepared during the synthesis of the marine benzosceptrin B. Conpounds inhibiting the RIPK1 protein kinase were discovered. A library of 54 synthetic analogs were prepared and evaluated through a phenotypic screen using the inhibition of the necrotic cell death induced by TNF-α in human Jurkat T cells deficient for the FADD protein. This article reports the design, synthesis and biological evaluation of a series of 2-aminobenzazoles on the necroptotic cell death through the inhibition of RIPK1 protein kinase. The 2-aminobenzimidazole and 2-aminobenzothiazole platforms presented herein can serve as novel chemical tools to study the molecular regulation of necroptosis and further develop lead drug candidates for chronic pathologies involving necroptosis.
Dithiocarbamate and CuO promoted one-pot synthesis of 2-(N-substituted)-aminobenzimidazoles and related heterocycles
Das, Parthasarathi,Kumar, C. Kiran,Kumar, K. Naresh,Innus,Iqbal, Javed,Srinivas, Nanduri
, p. 992 - 995 (2008/09/17)
A rapid and efficient one-pot method for the synthesis of 2-(N-substituted)-aminobenzimidazoles is described. The reaction is promoted by dithiocarbamate and catalytic CuO. This procedure is general and can be applied to synthesize many potential drug can
