765304-48-1Relevant academic research and scientific papers
In vitro activities of new 2-substituted quinolines against Leishmania donovani
Loiseau, Philippe M.,Gupta, Suman,Verma, Aditya,Srivastava, Saumya,Puri,Sliman, Faten,Normand-Bayle, Marie,Desmaele, Didier
scheme or table, p. 1777 - 1780 (2012/02/13)
A series of 9 quinolines and 18 styrylquinolines was evaluated for the drugs' in vitro antileishmanial activities and cytotoxicities. The 7-aroylstyrylquinoline scaffold appeared to be the most promising one, with the most interesting compound, no. 35, exhibiting a 50% inhibitory concentration (IC50) of 1.2 μM and a selectivity index value of 121.5. Compound 35 was 10-fold and 8-fold more active than miltefosine and sitamaquine, the reference compounds, with selectivity indexes 607-fold and 60-fold higher, respectively. Copyright
Identification and structure-activity relationship of 8-hydroxy-quinoline-7-carboxylic acid derivatives as inhibitors of Pim-1 kinase
Sliman, Faten,Blairvacq, Mélina,Durieu, Emilie,Meijer, Laurent,Rodrigo, Jordi,Desma?le, Didier
scheme or table, p. 2801 - 2805 (2010/07/05)
Pim-1 kinase is a cytoplasmic serine/threonine kinase that controls programmed cell death by phosphorylating substrates that regulate both apotosis and cellular metabolism. A series of 2-styrylquinolines and quinoline-2-carboxamides has been identified as potent inhibitors of the Pim-1 kinase. The 8-hydroxy-quinoline 7-carboxylic acid moiety appeared to be a crucial pharmacophore for activity. Molecular modeling indicated that interaction of this scaffold with Asp186 and Lys67 residues within the ATP-binding pocket might be responsible for the kinase inhibitory potency.
