References of "Counerotte, Stéphane"
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See detailValidation analytique d'une méthode chromatographique destinée à rechercher et à identifier les opiacés naturels ou (semi) synthétiques
DUBOIS, Nathalie ULg; Counerotte, Stéphane ULg; Goffin, Eric ULg et al

in Annales de Biologie Clinique (2014), 72(2), 197-206

L’identification de la substance absorbée par un consommateur d’opiacés peut être problématique dans la mesure où il n’existe pas de biomarqueur spécifique pour toutes les molécules. Nous avons développé ... [more ▼]

L’identification de la substance absorbée par un consommateur d’opiacés peut être problématique dans la mesure où il n’existe pas de biomarqueur spécifique pour toutes les molécules. Nous avons développé une technique de chromatographie liquide ultra-haute pression couplée à un spectromètre de masse en tandem qui permet l’identification et le dosage de 25 opiacés dans le plasma. La préparation de l’échantillon consiste en une extraction en phase solide sur colonnes Oasis ® MCX (Waters). La méthode a été validée selon les critères préconisés par la FDA, complètement pour 21 substances et avec quelques réserves pour les 4 produits restants. Cette méthode a été appliquée à 80 patients traités au CHU de Liège pour lesquels la recherche d’opiacés était positive. L’identification du produit consommé a été effective dans 86 % des cas. [less ▲]

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See detail6-Substituted 2-Oxo-2h-1-Benzopyran-3-Carboxylic Acid Derivatives in a New Approach of the Treatment of Cancer Cell Invasion and Metastasis
Kempen, I.; Hemmer, Marc ULg; Counerotte, Stéphane ULg et al

in European Journal of Medicinal Chemistry (2008), 43(12), 2735-50

Novel 6-substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives were synthesized and their potency in reducing the invasive behaviour of HT 1080 fibrosarcoma cells was evaluated. Structure ... [more ▼]

Novel 6-substituted 2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives were synthesized and their potency in reducing the invasive behaviour of HT 1080 fibrosarcoma cells was evaluated. Structure-activity relationships were deduced from biological results and will be used in further design of new active compounds. In particular, the acetoxymethyl substituent found at the 6-position of previously described active compounds can be replaced by an acetamidomethyl substituent without loss of potency; while the presence of an aryl ester function at the 3-position was preferred to a thioester or an amide function to induce marked biological activity. This work confirms the interest of aryl esters of 6-substituted coumarin-3-carboxylic acids as potential new anti-cancer agents. [less ▲]

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See detailIn Search of Novel Ampa Potentiators
Francotte, Pierre ULg; De Tullio, Pascal ULg; Fraikin, Pierre ULg et al

in Recent Patents on CNS Drug Discovery (2006), 1(3), 239-46

Glutamate is the major excitatory neurotransmitter in the brain. Amongst ionotropic receptors responding to glutamate, the AMPA subtype has been considered as essential for the fast excitatory ... [more ▼]

Glutamate is the major excitatory neurotransmitter in the brain. Amongst ionotropic receptors responding to glutamate, the AMPA subtype has been considered as essential for the fast excitatory neurotransmission in the central nervous system and the expression and maintenance of long-term potentiation. As glutamate is known to be involved in many neurological and psychiatric disorders, AMPA receptors seem to represent interesting targets to develop therapeutic drugs. Hence, the enhancement of AMPA signals is an approach currently investigated for the management of Alzheimer's disease, schizophrenia or mood disorders. In particular, many efforts are being conducted in the development of AMPA positive allosteric modulators ("potentiators"), which alter the rate of receptor desensitization. The major chemical families developed as AMPA potentiators are aniracetam derivatives, cyclothiazide derivatives and biarylpropylsulfonamides derivatives. [less ▲]

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See detailEffect on KATP channel activation properties and tissue selctivity of the nature of the substituent in the 7- and the 3-position of 4H-1,2,4-benzothiadiazine
Boverie, S.; Antoine, M.-H.; Somers, F. et al

in Journal of Medicinal Chemistry (2005), 48

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See detail3-Bromophenyl 6-acetoxymethyl-2-oxo-2H-1-benzopyran-3-carboxylate inhibits cancer cell invasion in vitro and tumour growth in vivo
Kempen, I.; Papapostolou, D.; Thierry, N. 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 ▲]

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See detailEffects on in vitro and in vivo cellular invasion of two 6-(acetoxymethyl)-2-oxo-2H-1-benzopyran-3-carboxylic acid derivatives
Kempen, I.; Pochet, L.; Papapostolou, D. et al

Poster (2001, October 16)

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