One- or Two-Step Synthesis of C-8 and N-9 Substituted Purines

Autor: Laurent Dubuquoy, Mélanie Bollier, Régis Millet, Nathalie Azaroual, Natascha Leleu-Chavain, Perrine Six, Frédérique Klupsch

Publikováno v: The Journal of organic chemistry. 83(1)

A novel and original strategy to obtain rapidly a large diversity of C-8 and N-9 substituted purines was developed. The present procedure describes annulation reactions in one or two steps starting from 5-aminoimidazole-4-carbonitriles 1–8 in moder

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c287f9f5b690cb556199b6abdc9e619a
https://pubmed.ncbi.nlm.nih.gov/29192784

New selective carbonic anhydrase IX inhibitors: Synthesis and pharmacological evaluation of diarylpyrazole-benzenesulfonamides

Autor: Samuel Meignan, Abigaëlle Gros, Tiphaine Rogez-Florent, Amélie Lansiaux, Catherine Foulon, Jean François Goossens, Raphaël Frédérick, Sebastien Gluszok, Bernard Masereel, Laurence Goossens, Perrine Six, Claudiu T. Supuran, Christine Bal-Mahieu, Andrea Scozzafava, Patrick Depreux

Publikováno v: Bioorganic & Medicinal Chemistry
Bioorganic & Medicinal Chemistry : the tetrahedron journal for research at the interface of chemistry and biology, Vol. 21, no. 6, p. 1451-1464 (2013)
Bioorganic & Medicinal Chemistry; Vol 21
Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry, Elsevier, 2013, 21 (6), pp.1451-1464. ⟨10.1016/j.bmc.2012.10.029⟩

Carbonic anhydrase (CA) IX expression is increased upon hypoxia and has been proposed as a therapeutic target since it has been associated with poor prognosis, tumor progression and pH regulation. We report the synthesis and the pharmacological evalu

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d24fc0ffbfbf6b174096e2e6e1a78a94

Novel and Efficient One-Pot Synthesis of (Aminophenyl)carbamic Acid Esters

Autor: Laurence Goossens, Patrick Depreux, Perrine Six, Nicolas Lebegue, Antonio Garofalo

Publikováno v: Synthetic Communications. 41:2007-2016

A novel and efficient protocol is developed for the synthesis of various (aminophenyl)carbamic acid esters from the reduction and condensation of nitrophenyl isocyanate derivatives. The reaction takes place in various hydroxy derivatives such as alco

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::674c844e03002294e181441c414e1b32
https://doi.org/10.1080/00397911.2010.494818

Synthesis and Antiproliferative Activity of 2-amino-4-Anilinoquinazoline Derivatives

Autor: Patrick Depreux, Ravez S, Laurence Goossens, Arsenlis S, Castillo Aguilera O, Baldeyrou B, Lansiaux A, Schifano-Faux N, Barczyk A, Jean-François Goossens, Perrine Six

Publikováno v: Medicinal Chemistry. 5

Recently, we have reported a series of 4-anilino-6,7-dimethoxyquinazolines as tyrosine kinase inhibitors with interesting in vitro IC50 values for the Epidermal Growth Factor Receptor (EGFR) and/or for the Vascular Endothelial Growth Factor Receptor-

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::ed244a2b5f1b7c641f45005415767376
https://doi.org/10.4172/2161-0444.1000245

Label-free characterization of carbonic anhydrase-novel inhibitor interactions using surface plasmon resonance, isothermal titration calorimetry and fluorescence-based thermal shift assays

Autor: Tiphaine, Rogez-Florent, Laetitia, Duhamel, Laurence, Goossens, Perrine, Six, Anne-Sophie, Drucbert, Patrick, Depreux, Pierre-Marie, Danzé, David, Landy, Jean-François, Goossens, Catherine, Foulon

Publikováno v: Journal of molecular recognition : JMR. 27(1)

This work describes the development of biophysical unbiased methods to study the interactions between new designed compounds and carbonic anhydrase II (CAII) enzyme. These methods have to permit both a screening of a series of sulfonamide derivatives

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::d4093be140eb3cc00f0a3f0e0f7e0df2
https://pubmed.ncbi.nlm.nih.gov/24375583