Search

Your search keyword '"Bourin, Arnaud"' showing total 12 results
Start Over Author "Bourin, Arnaud"
12 results on '"Bourin, Arnaud"'

1. Treatment of Intestinal Fibrosis in Experimental Inflammatory Bowel Disease by the Pleiotropic Actions of a Local Rho Kinase Inhibitor

Author

Holvoet, Tom, Devriese, Sarah, Castermans, Karolien, Boland, Sandro, Leysen, Dirk, Vandewynckel, Yves-Paul, Devisscher, Lindsey, Van den Bossche, Lien, Van Welden, Sophie, Dullaers, Melissa, Vandenbroucke, Roosmarijn E., De Rycke, Riet, Geboes, Karel, Bourin, Arnaud, Defert, Olivier, Hindryckx, Pieter, De Vos, Martine, and Laukens, Debby

Published
2017
Full Text
View/download PDF

2. Abstract 53: Discovery of novel potent and orally bioavailable small-molecule inhibitors of ENPP1 to stabilize cGAMP and ATP in the tumor microenvironment and boost anti-tumor immunity

Author

Versele, Matthias, primary, del Pino Garcia, Javier, additional, Vandecaetsbeek, Ilse, additional, Castermans, Karolien, additional, Kellens, Ranie, additional, Haeck, Wanda, additional, Klaassen, Hugo, additional, Bourin, Arnaud, additional, De Clercq, Dries, additional, Allasia, Sara, additional, Boland, Sandro, additional, Marchand, Arnaud, additional, Chaltin, Patrick, additional, and Bollen, Mathieu, additional

Published
2021
Full Text
View/download PDF

5. Drug to Genome to Drug: Discovery of New Antiplasmodial Compounds

Author

Beghyn, Terence B., Charton, Julie, Leroux, Florence, Laconde, Guillaume, Bourin, Arnaud, Cos, Paul, Maes, Louis, and Deprez, Benoit

Abstract

The dominant strategy for discovery of new antimalarial drugs relies on cell-free assays on specific biochemical pathways of Plasmodium falciparum. However, it appears that screening directly on the parasite is a more rewarding approach. The “drug to genome to drug” approach consists of testing a small set of structural analogues of a drug acting on human proteins that have plasmodial orthologues. Both man and plasmodium possess cyclic nucleotide phosphodiesterases (PDEs) that are key players of cell homeostasis. We synthesized and tested 40 analogues of tadalafil, a human PDE5 inhibitor, on P. falciparumin culture and obtained potent inhibitors of parasite growth. We discuss the structure−activity relationships, which support the hypothesis that our compounds kill the parasite via inhibition of plasmodial PDE activity. We also prove that antiplasmodial derivatives inhibit the hydrolysis of cyclic nucleotides of the parasite, validating the cAMP/cGMP pathways as therapeutic targets against Plasmodium falciparum.

Published
2024
Full Text
View/download PDF

7. Design, Synthesis, and Biological Evaluation of Novel, Highly Active Soft ROCK Inhibitors

Author

Boland, Sandro, primary, Bourin, Arnaud, additional, Alen, Jo, additional, Geraets, Jacques, additional, Schroeders, Pieter, additional, Castermans, Karolien, additional, Kindt, Nele, additional, Boumans, Nicki, additional, Panitti, Laura, additional, Fransen, Silke, additional, Vanormelingen, Jessica, additional, Stassen, Jean Marie, additional, Leysen, Dirk, additional, and Defert, Olivier, additional

Published
2015
Full Text
View/download PDF

12. Total synthesis of discodermolide: optimization of the effective synthetic route.

Author

de Lemos E, Porée FH, Bourin A, Barbion J, Agouridas E, Lannou MI, Commerçon A, Betzer JF, Pancrazi A, and Ardisson J

Subjects
Alcohols, Alkenes, Antineoplastic Agents, Tubulin Modulators, Alkanes chemical synthesis, Carbamates chemical synthesis, Lactones chemical synthesis, Pyrones chemical synthesis
Abstract

An efficient and modulable total synthesis of discodermolide (DDM), a unique marine anticancer polyketide is described including related alternative synthetic approaches. Particularly notable is the repeated application of a crotyltitanation reaction to yield homoallylic (Z)-O-ene-carbamate alcohols with excellent selectivity. Advantage was taken of this reaction not only for the stereocontrolled building of the syn-anti methyl-hydroxy-methyl triads of DDM, but also for the direct construction of the terminal (Z)-diene. Of particular interest is also the installation of the C13=C14 (Z)-double bond through a highly selective dyotropic rearrangement. The preparation of the middle C8-C14 fragment in two sequential stages and its coupling to the C1-C7 moiety was a real challenge and required careful optimization. Several synthetic routes were explored to allow high and reliable yields. Due to the flexibility and robust character of this approach, it might enable a systematic structural variation of DDM and, therefore, the elaboration and exploration of novel discodermolide structural analogues.

Published
2008
Full Text
View/download PDF

Catalog

Books, media, physical & digital resources
See catalog results