98588-66-0Relevant academic research and scientific papers
Identification of Eukaryotic Translation Elongation Factor 1-α 1 Gamendazole-Binding Site for Binding of 3-Hydroxy-4(1 H)-quinolinones as Novel Ligands with Anticancer Activity
Burglová, Kristyna,Rylová, Gabriela,Markos, Athanasios,Prichystalova, Hana,Soural, Miroslav,Petracek, Marek,Medvedikova, Martina,Tejral, Gracian,Sopko, Bruno,Hradil, Pavel,Dzubak, Petr,Hajduch, Marian,Hlavac, Jan
, p. 3027 - 3036 (2018)
Here, we have identified the interaction site of the contraceptive drug gamendazole using computational modeling. The drug was previously described as a ligand for eukaryotic translation elongation factor 1-α 1 (eEF1A1) and found to be a potential target site for derivatives of 2-phenyl-3-hydroxy-4(1H)-quinolinones (3-HQs), which exhibit anticancer activity. The interaction of this class of derivatives of 3-HQs with eEF1A1 inside cancer cells was confirmed via pull-down assay. We designed and synthesized a new family of 3-HQs and subsequently applied isothermal titration calorimetry to show that these compounds strongly bind to eEF1A1. Further, we found that some of these derivatives possess significant in vitro anticancer activity.
Electrosynthesis of aryl-carboxylic acids from chlorobenzene derivatives and carbon dioxide
Heintz, Monique,Sock, Oumar,Saboureau, Christophe,Perichon, Jacques,Troupel, Michel
, p. 1631 - 1636 (2007/10/02)
The electrocarboxylation of a large variety of chlorobenzenic compounds is achieved in N,N-dimethylformamide by constant current electrolysis between a stainless steel cathode and a sacrificial magnesium anode in a diaphragmless cell. Substituted benzoic acids are obtained in high yield in simle conditions thus avoiding the usual preparation of organometallic intermediates.
