References of "Pochet, L"
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See detailIs thrombin generation the new rapid, reliable and relevant pharmacological tool for the development of anticoagulant drugs?
Robert, S.; Ghiotto, J.; Pirotte, Bernard ULg et al

Conference (2009, November)

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See detailIs thrombin generation the new rapid, reliable and relevant pharmacological tool for the development of anticoagulant drugs ?
Robert, S.; Ghiotto, J.; Pirotte, Bernard ULg et al

in Pharmacological Research (2009), 59

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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 detailSynthesis and pharmacological evaluation of a new targeted drug carrier system: β-Cyclodextrin coupled to oxytocin
Bertolla, C; Rolin, S; Evrard, Brigitte ULg et al

in Bioorganic & Medicinal Chemistry Letters (2008), 18

β-Cyclodextrin (β-CD) was monofunctionalized into its carboxylic derivative and then conjugated to the N-side of oxytocin (OT), a nonapeptide involved in human behavior and myometrium contraction. On ... [more ▼]

β-Cyclodextrin (β-CD) was monofunctionalized into its carboxylic derivative and then conjugated to the N-side of oxytocin (OT), a nonapeptide involved in human behavior and myometrium contraction. On isolated rat myometrium, this conjugate (β-CD-OT) partly preserves the contracting activity of OT (EC50 = 0.40 μM vs 1.7 nM). Moreover, the contraction induced frequency is also lowered by β-CD-OT. This novel hydrophilic targeted carrier could form a host–guest complex with prostaglandins and their derivatives used as labor inducers or with anticancer drugs used in cervix and endometrial cancer. This strategy can improve the solubility, the stability, and/or the biological activity of these drugs as well as reducing their side-effects. [less ▲]

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See detailThrombin activity profile: a rapid, reliable and relevant ex vivo screening test for the development of anticoagulant drugs
Robert, S.; Ghiotto, J.; Pirotte, Bernard ULg et al

Conference (2007, October)

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See detailThrombin activity profile : a powerful ex vivo screening test for the development of anticoagulant drugs
Robert, S.; Ghiotto, J.; Pirotte, Bernard ULg et al

Poster (2007, July)

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See detail3,6-Disubstitued coumarins as mechanism-based inhibitors of thrombin and factor Xa
Frederick, R.; Robert, S.; Charlier, C. et al

in Journal of Medicinal Chemistry (2005), 48

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See detailSynthèse et évaluation biologique de nouvelles coumarines en tant qu’anticoagulants potentiels
Pochet, L.; Rolin, S.; Morel, M. et al

Poster (2003, May)

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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 detailInvestigation of the inhibition mechanism of coumarins on chymotrypsin by mass spectrometry
Pochet, L.; Dieu, M.; Frederick, R. et al

in Tetrahedron (2003)

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See detailDesign et synthèse de nouveaux dérivés coumariniques inhibiteurs de thrombine
Frederick, R.; Pochet, L.; Pirotte, Bernard ULg et al

Poster (2002, May 31)

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See detailStructural approach of the mechanism of inhibition of -chymotrypsin by coumarins
Wouters, J.; Huygens, M.; Pochet, L. et al

in Bioorganic & Medicinal Chemistry Letters (2002), 12

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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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See detailInhibition of thrombin by oxobenzopyran derivatives: structure-activity relationships
Kibirev, V. K.; Lacan, F.; Bourdel, F. et al

Poster (2001, July)

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See detailSynthèse et évaluation enzymatique de nouvelles coumarines en tant qu’inhibiteurs de thrombine
Pochet, L.; Doucet, C.; Pirotte, Bernard ULg et al

Poster (2001, June 01)

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See detailEffects on cellular invasion of two synthetic coumarins
Kempen, I.; Papapostolou, D.; Pochet, L. et al

Conference (2001, May)

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

Poster (2001, April 21)

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