Coumarinic derivatives show anti-inflamatory effects on alveolor macrophages, but their anti-elastase activity is essential to reduce lung inflammation in vivo; ; et al in International Immunopharmacology (2009), 9 Detailed reference viewed: 25 (4 ULg) Towards the control of intercellular protein turnover: Mitochondrial Lon protease inhibitors versus proteasome inhibitors; ; et al in Biochimie (2008), 90 Detailed reference viewed: 14 (3 ULg) 3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo; ; et al in British Journal of Cancer (2003), 88(7), 1111-1118 In search for new anticancer agents, we have evaluated the antiinvasive and antimigrative properties of recently developed synthetic coumarin derivatives among which two compounds revealed important ... [more ▼] In search for new anticancer agents, we have evaluated the antiinvasive and antimigrative properties of recently developed synthetic coumarin derivatives among which two compounds revealed important activity: 3-chlorophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate and 3-bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate, Both drugs were able to inhibit cell invasion markedly in a Boyden chamber assay, the bromo derivative being more potent than the reference matrix metalloprotease (MMP) inhibitor GI 129471. In vivo, tumour growth was reduced when nude mice grafted with HT 1080 or MDA-MB231 cells were treated i.p. 3 days week(-1) with the bromo coumarin derivative. These effects were not associated with the inhibition of urokinase, plasmin, MMP-2 or MMP-9. The mechanism of action of the drugs remains to be elucidated. However, these two coumarin derivatives may serve as new lead compounds of an original class of antitumour agents. [less ▲] Detailed reference viewed: 26 (7 ULg) Design et synthèse de nouveaux dérivés coumariniques inhibiteurs de thrombine; ; Pirotte, Bernard et alPoster (2002, May 31) Detailed reference viewed: 3 (1 ULg) Effects on in vitro and in vivo cellular invasion of two 6-(acetoxymethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives; ; et al Poster (2001, October 16) Detailed reference viewed: 2 (0 ULg) Inhibition of thrombin by oxobenzopyran derivatives: structure-activity relationships; ; et al Poster (2001, July) Detailed reference viewed: 6 (0 ULg) Comparaison de l’effet de deux dérivés de l’acide 6-(acetoxymethyl)-2-oxo-2H-1-benzopyrane-3-carboxylique sur l’inhibition de l’invasion cellulaire in vitro et in vivo; ; et al Poster (2001, June 01) Detailed reference viewed: 2 (0 ULg) Synthèse et évaluation enzymatique de nouvelles coumarines en tant qu’inhibiteurs de thrombine; ; Pirotte, Bernard et alPoster (2001, June 01) Detailed reference viewed: 5 (0 ULg) Inhibition mechanism of serine protease by coumarin derivatives; ; et al Conference (2001, May) Detailed reference viewed: 39 (0 ULg) Effects on cellular invasion of two synthetic coumarins; ; et al Conference (2001, May) Detailed reference viewed: 6 (1 ULg) Effects on cellular invasion of 6-(acetoxymethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives; ; et al Poster (2001, April 21) Detailed reference viewed: 3 (0 ULg) Comparaison de l’effet de deux coumarines sur l’inhibition de l’invasion cellulaire in vitro et in vivo; ; et al Poster (2001, January 26) Detailed reference viewed: 1 (0 ULg) Inhibition of cellular invasion by 3-chlorophenyl 6-(acetoxymethyl)-2-oxo-2H-1-benzopyran-3-carboxylate; ; et al Poster (2000, September) Detailed reference viewed: 1 (0 ULg) Oxobenzopyran derivatives as thrombin inhibitors; ; et al Poster (2000, September) Detailed reference viewed: 1 (0 ULg) Specific inhibitors of human leukocyte elastase; ; et al Poster (2000, August) Detailed reference viewed: 3 (0 ULg) Activity and inhibition mechanism of coumarin-based derivatives as protease inhibitor; ; et al Poster (2000, June) Detailed reference viewed: 3 (0 ULg) Le 6-(acetoxymethyl)-2-oxo-2H-1-benzopyrane-3-carboxylate de 3-chlorophényle agissant en tant qu’inhibiteur potentiel de l’invasion tumorale; ; et al Poster (2000, May) Detailed reference viewed: 10 (0 ULg) Inhibition of cancer cells invasion by coumarin derivatives; ; et al Poster (2000, January 29) Detailed reference viewed: 2 (0 ULg) Les esters de l’acide 6-(acétoxyméthyl)-2-oxo-2H-1-benzopyrane-3-carboxylique en tant qu’agents antiinvasifs potentiels dans le traitement du cancer; ; et al Conference (2000, January 28) Detailed reference viewed: 2 (0 ULg) Les esters de l’acide 6-(acétoxyméthyl)-2-oxo-2H-1-benzopyrane-3-carboxylique en tant qu’agents antiinvasifs potentiels dans le traitement du cancer; ; et al Poster (2000, January 28) Detailed reference viewed: 3 (0 ULg) |
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