475098-86-3Relevant articles and documents
Investigating the antiproliferative activity of quinoline-5,8-diones and styrylquinolinecarboxylic acids on tumor cell lines
Podeszwa,Niedbala,Polanski,Musiol,Tabak,Finster,Serafin,Milczarek,Wietrzyk,Boryczka,Mol,Jampilek,Dohnal,Kalinowski,Richardson
, p. 6138 - 6141 (2007)
The structure-activity relationships of new quinoline based compounds were investigated. Quinoline-5,8-dione and styrylquinoline scaffolds were used for the design of potentially active compounds. The novel analogues had comparable antiproliferative activ
Quinoline-galactose hybrids bind selectively with high affinity to a galectin-8 N-terminal domain
Pal, Kumar Bhaskar,Mahanti, Mukul,Huang, Xiaoli,Persson, Stella,Sundin, Anders P.,Zetterberg, Fredrik R.,Oredsson, Stina,Leffler, Hakon,Nilsson, Ulf J.
, p. 6295 - 6305 (2018/09/10)
Quinolines, indolizines, and coumarins are well known structural elements in many biologically active molecules. In this report, we have developed straightforward methods to incorporate quinoline, indolizine, and coumarin structures into galactoside derivatives under robust reaction conditions for the discovery of glycomimetic inhibitors of the galectin family of proteins that are involved in immunological and tumor-promoting biological processes. Evaluation of the quinoline, indolizine and coumarin-derivatised galactosides as inhibitors of the human galectin-1, 2, 3, 4N (N-terminal domain), 4C (C-terminal domain), 7, 8N, 8C, 9N, and 9C revealed quinoline derivatives that selectively bound galectin-8N, a galectin with key roles in lymphangiogenesis, tumor progression, and autophagy, with up to nearly 60-fold affinity improvements relative to methyl β-d-galactopyranoside. Molecular dynamics simulations proposed an interaction mode in which Arg59 had moved 2.5 ? and in which an inhibitor carboxylate and quinoline nitrogen formed structure-stabilizing water-mediated hydrogen bonds. The compounds were demonstrated to be non-toxic in an MTT assay with several breast cancer cell lines and one normal cell line. The improved affinity, selectivity, and low cytotoxicity suggest that the quinoline-galactoside derivatives provide an attractive starting point for the development of galectin-8N inhibitors potentially interfering with pathological lymphangiogenesis, autophagy, and tumor progression.
TRIAZOLOPYRIDINE COMPOUNDS AS PIM KINASE INHIBITORS
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Page/Page column 88, (2012/12/13)
Compounds of Formula I: in which R1, R2, R3, R4 and R10 have the meanings given in the specification, are receptor tyrosine inhibitors useful in the treatment of diseases mediated by PIM-1 and/or PIM-2 and/or PIM-3 kinases.
Use of the Kohonen neural network for rapid screening of ex vivo anti-HIV activity of styrylquinolines
Polanski, Jaroslaw,Zouhiri, Fatima,Jeanson, Laurence,Desma?le, Didier,D'Angelo, Jean,Mouscadet, Jean-Fran?ois,Gieleciak, Rafal,Gasteiger, Johann,Le Bret, Marc
, p. 4647 - 4654 (2007/10/03)
Using the Kohonen neural network, the electrostatic potentials on the molecular surfaces of 14 styrylquinoline derivatives were drawn as comparative two-dimensional maps and compared with their known human immunodeficiency virus (HIV)-1 replication blocki
