Novel library synthesis of 3,4-disubstituted pyridin-2(1H)-ones via cleavage of pyridine-2-oxy-7-azabenzotriazole ethers under ionic hydrogenation conditions at room temperature

Autor: Romain Pierre, Anne Brethon, Sylvain A. Jacques, Aurélie Blond, Sandrine Chambon, Sandrine Talano, Catherine Raffin, Branislav Musicki, Claire Bouix-Peter, Loic Tomas, Gilles Ouvry, Rémy Morgentin, Laurent F. Hennequin, Craig S. Harris

Publikováno v: Beilstein Journal of Organic Chemistry, Vol 17, Iss 1, Pp 156-165 (2021)

In our hands, efficient access to the 4-amino-3-carboxamide disubstituted pyridine-2(1H)-one kinase hinge-binder motif proved to be more challenging than anticipated requiring a significant investment in route scouting and optimization. This full pap

Externí odkaz: https://doaj.org/article/2acdd653d9364f4c95c1ad7741ba07ae

Inhibition of the NAD salvage pathway in schistosomes impairs metabolism, reproduction, and parasite survival

Autor: Jeremy B. Foote, Hélène Muller-Steffner, Davide Botta, Sylvain A. Jacques, Leonardo Sorci, Frances E. Lund, Tulin Dadali, Michael D. Schultz, Esther Kellenberger

Publikováno v: PLoS Pathogens
PLoS Pathogens, Public Library of Science, 2020, 16 (5), pp.e1008539. ⟨10.1371/journal.ppat.1008539⟩
PLoS Pathogens, Vol 16, Iss 5, p e1008539 (2020)

NAD, a key co-enzyme required for cell metabolism, is synthesized via two pathways in most organisms. Since schistosomes apparently lack enzymes required for de novo NAD biosynthesis, we evaluated whether these parasites, which infect >200 million pe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c20ecca6a432763778842c9c459bf2b9
https://hal.archives-ouvertes.fr/hal-03021592

Corrigendum: MTH1 inhibition eradicates cancer by preventing sanitation of the dNTP pool

Autor: Helge, Gad, Tobias, Koolmeister, Ann-Sofie, Jemth, Saeed, Eshtad, Sylvain A, Jacques, Cecilia E, Ström, Linda M, Svensson, Niklas, Schultz, Thomas, Lundbäck, Berglind Osk, Einarsdottir, Aljona, Saleh, Camilla, Göktürk, Pawel, Baranczewski, Richard, Svensson, Ronnie P-A, Berntsson, Robert, Gustafsson, Kia, Strömberg, Kumar, Sanjiv, Marie-Caroline, Jacques-Cordonnier, Matthieu, Desroses, Anna-Lena, Gustavsson, Roger, Olofsson, Fredrik, Johansson, Evert J, Homan, Olga, Loseva, Lars, Bräutigam, Lars, Johansson, Andreas, Höglund, Anna, Hagenkort, Therese, Pham, Mikael, Altun, Fabienne Z, Gaugaz, Svante, Vikingsson, Bastiaan, Evers, Martin, Henriksson, Karl S A, Vallin, Olov A, Wallner, Lars G J, Hammarström, Elisee, Wiita, Ingrid, Almlöf, Christina, Kalderén, Hanna, Axelsson, Tatjana, Djureinovic, Jordi, Carreras Puigvert, Maria, Häggblad, Fredrik, Jeppsson, Ulf, Martens, Cecilia, Lundin, Bo, Lundgren, Ingrid, Granelli, Annika, Jenmalm Jensen, Per, Artursson, Jonas A, Nilsson, Pål, Stenmark, Martin, Scobie

Publikováno v: Nature. 544(7651)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::a849c4dcef26131d22c77ff42f3cbc8e
https://pubmed.ncbi.nlm.nih.gov/24695224

A facile and efficient synthesis of tetrahydro-β-carbolines

Autor: Marie-Caroline Jacques-Cordonnier, Sabin Llona-Minguez, Armando Cázares-Körner, Martin Scobie, Sylvain A. Jacques, Thomas Helleday, Matthieu Desroses, Tobias Koolmeister

Publikováno v: Tetrahedron Letters. 54:3554-3557

This Letter describes a convenient, efficient, and clean synthesis of various tetrahydro-β-carbolines catalyzed by propane phosphonic acid anhydride T3P® under microwave irradiation.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::d5c9639dca6250d7f14dbfae8a9c78b9
https://doi.org/10.1016/j.tetlet.2013.04.107

Studies on the Total Synthesis of Lactonamycin: Synthesis of the Fused Pentacyclic B-F Ring Unit

Autor: Andrew J. P. White, Andreas Blum, Anthony G. M. Barrett, Björn Gebhardt, Nathalie Lebrasseur, Igor Larrosa, Sylvain A. Jacques, Simon Michaelis

Publikováno v: European Journal of Organic Chemistry. 2012:107-113

This paper describes an approach towards the total synthesis of lactonamycin with the elaboration of a key pentacyclic unit. Key steps include the synthesis of benzyl bromide 8 in eight steps and 23 % overall yield starting from 4-methoxyphenol; a hi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::c4c166887ae8fbe7946cd2253a10ee98
https://doi.org/10.1002/ejoc.201101317