Search Results - "Dousson, Cyril"

Is there any need for new, long-acting nucleos(t)ide analogues for the treatment of hepatitis B infection? by Durantel, David, Dousson, Cyril B., Lampertico, Pietro

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Current and future use of nucleo(s)tide prodrugs in the treatment of hepatitis C virus infection by Dousson, Cyril B

“…This review describes the current state of discovery of past most important nucleoside and nucleotide prodrugs in the treatment of hepatitis C virus infection…”
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HBV replication inhibitors by Pierra Rouviere, Claire, Dousson, Cyril B., Tavis, John E.

“…Chronic Hepatitis B Virus infections afflict >250 million people and kill nearly 1 million annually. Current non-curative therapies are dominated by…”
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Synthesis and Biological Evaluation of Aryl-phospho-indole as Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors by Alexandre, François-René, Amador, Agnès, Bot, Stéphanie, Caillet, Catherine, Convard, Thierry, Jakubik, Jocelyn, Musiu, Chiara, Poddesu, Barbara, Vargiu, Luana, Liuzzi, Michel, Roland, Arlène, Seifer, Maria, Standring, David, Storer, Richard, Dousson, Cyril B

“…A novel series of 3-aryl-phospho-indole (API) non-nucleoside reverse transcriptase inhibitors of HIV-1 was developed. Chemical variation in the phosphorus…”
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The discovery of IDX21437: Design, synthesis and antiviral evaluation of 2′-α-chloro-2′-β-C-methyl branched uridine pronucleotides as potent liver-targeted HCV polymerase inhibitors by Alexandre, François-René, Badaroux, Eric, Bilello, John P., Bot, Stéphanie, Bouisset, Tony, Brandt, Guillaume, Cappelle, Sylvie, Chapron, Christopher, Chaves, Dominique, Convard, Thierry, Counor, Clément, Da Costa, Daniel, Dukhan, David, Gay, Marion, Gosselin, Gilles, Griffon, Jean-François, Gupta, Kusum, Hernandez-Santiago, Brenda, La Colla, Massimiliano, Lioure, Marie-Pierre, Milhau, Julien, Paparin, Jean-Laurent, Peyronnet, Jérôme, Parsy, Christophe, Pierra Rouvière, Claire, Rahali, Houcine, Rahali, Rachid, Salanson, Aurélien, Seifer, Maria, Serra, Ilaria, Standring, David, Surleraux, Dominique, Dousson, Cyril B.

“…[Display omitted] Herein we describe the discovery of IDX21437 35b, a novel RPd-aminoacid-based phosphoramidate prodrug of 2′-α-chloro-2′-β-C-methyluridine…”
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Synthesis and Antiviral Evaluation of Carbocyclic Nucleoside Analogs of Nucleoside Reverse Transcriptase Translocation Inhibitor MK-8591 (4′-Ethynyl-2-fluoro-2′-deoxyadenosine) by Alexandre, François-René, Rahali, Rachid, Rahali, Houcine, Guillon, Sandra, Convard, Thierry, Fillgrove, Kerry, Lai, Ming-Tain, Meillon, Jean-Christophe, Xu, Min, Small, James, Dousson, Cyril B, Raheem, Izzat T

“…MK-8591 (4′-ethynyl-2-fluoro-2′-deoxyadenosine) is a novel nucleoside analog that displays a differentiated mechanism of action as a nucleoside reverse…”
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Discovery of benzophosphadiazine drug candidate IDX375: A novel hepatitis C allosteric NS5B RdRp inhibitor by Paparin, Jean-Laurent, Amador, Agnès, Badaroux, Eric, Bot, Stéphanie, Caillet, Catherine, Convard, Thierry, Da Costa, Daniel, Dukhan, David, Griffe, Ludovic, Griffon, Jean-François, LaColla, Massimiliano, Leroy, Frédéric, Liuzzi, Michel, Giulia Loi, Anna, McCarville, Joe, Mascia, Valeria, Milhau, Julien, Onidi, Loredana, Pierra, Claire, Rahali, Rachid, Rosinosky, Elodie, Sais, Efisio, Seifer, Maria, Surleraux, Dominique, Standring, David, Dousson, Cyril B.

“…[Display omitted] Hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent…”
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Development and Scale-Up of a Manufacturing Route for the Non-nucleoside Reverse Transcriptase Inhibitor GSK2248761A (IDX-899): Synthesis of an Advanced Key Chiral Intermediate by Bellingham, Richard, Borrett, Gary, Bret, Guillaume, Choudary, Bernadette, Colclough, David, Hayes, Jerome, Hayler, John, Hodnett, Neil, Ironmonger, Alan, Ochen, Augustine, Pascoe, David, Richardson, John, Vit, Erica, Alexandre, François-René, Caillet, Catherine, Amador, Agnès, Bot, Stéphanie, Bonaric, Séverine, da Costa, Daniel, Lioure, Marie-Pierre, Roland, Arlène, Rosinovsky, Elodie, Parsy, Christophe, Dousson, Cyril B

“…A new and improved synthetic route to an intermediate in the synthesis of the phosphinate ester GSK2248761A is described. In the key step, we describe the…”
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A highly diastereoselective chloride-mediated dynamic kinetic resolution at phosphorus on-route to a key intermediate in the synthesis of GSK2248761A by Ironmonger, Alan, Shipton, Mark, Slater, Fiona, Szeto, Pete, Unthank, Matthew G., Alexandre, François-René, Caillet, Catherine, Dousson, Cyril B.

“…[Display omitted] •Stereoselective phosphinate esters synthesis.•Highest diastereoselectivity using a phenyl glycinamide derivative.•Isolated in 81% yield,…”
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Novel methods for the synthesis of 1,5,2-diazaphosphinines as potential inhibitors of HCV polymerase by Da Costa, Daniel, Roland, Arlène, Dousson, Cyril B.

“…[Display omitted] •Two new methods for the preparation of the 1,5,2-diazaphosphinines are described.•The 1,5,2-diazaphosphinines are new HCV NS5B…”
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Discovery of the Aryl-phospho-indole IDX899, a Highly Potent Anti-HIV Non-nucleoside Reverse Transcriptase Inhibitor by Dousson, Cyril, Alexandre, François-René, Amador, Agnès, Bonaric, Séverine, Bot, Stéphanie, Caillet, Catherine, Convard, Thierry, da Costa, Daniel, Lioure, Marie-Pierre, Roland, Arlène, Rosinovsky, Elodie, Maldonado, Sébastien, Parsy, Christophe, Trochet, Christophe, Storer, Richard, Stewart, Alistair, Wang, Jingyang, Mayes, Benjamin A, Musiu, Chiara, Poddesu, Barbara, Vargiu, Luana, Liuzzi, Michel, Moussa, Adel, Jakubik, Jocelyn, Hubbard, Luke, Seifer, Maria, Standring, David

“…Here, we describe the design, synthesis, biological evaluation, and identification of a clinical candidate non-nucleoside reverse transcriptase inhibitors…”
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Discovery, Synthesis, and in Vivo Activity of a New Class of Pyrazoloquinazolines as Selective Inhibitors of Aurora B Kinase by Mortlock, Andrew A, Foote, Kevin M, Heron, Nicola M, Jung, Frédéric H, Pasquet, Georges, Lohmann, Jean-Jacques M, Warin, Nicolas, Renaud, Fabrice, De Savi, Chris, Roberts, Nicola J, Johnson, Trevor, Dousson, Cyril B, Hill, George B, Perkins, David, Hatter, Glenn, Wilkinson, Robert W, Wedge, Stephen R, Heaton, Simon P, Odedra, Rajesh, Keen, Nicholas J, Crafter, Claire, Brown, Elaine, Thompson, Katherine, Brightwell, Stephen, Khatri, Liz, Brady, Madeleine C, Kearney, Sarah, McKillop, David, Rhead, Steve, Parry, Tony, Green, Stephen

“…The Aurora kinases have been the subject of considerable interest as targets for the development of new anticancer agents. While evidence suggests inhibition…”
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Synthesis of potent and broad genotypically active NS5B HCV non-nucleoside inhibitors binding to the thumb domain allosteric site 2 of the viral polymerase by Pierra Rouvière, Claire, Amador, Agnès, Badaroux, Eric, Convard, Thierry, Da Costa, Daniel, Dukhan, David, Griffe, Ludovic, Griffon, Jean-François, LaColla, Massimiliano, Leroy, Frédéric, Liuzzi, Michel, Loi, Anna Giulia, McCarville, Joe, Mascia, Valeria, Milhau, Julien, Onidi, Loredana, Paparin, Jean-Laurent, Rahali, Rachid, Sais, Efisio, Seifer, Maria, Surleraux, Dominique, Standring, David, Dousson, Cyril

“…[Display omitted] The hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional…”
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Asymmetric hydrogenation reactions mediated by a new class of bicyclic bisphosphinites by Derrien, Nadine, Dousson, Cyril B., Roberts, Stanley M., Berens, Ulrich, Burk, Mark J., Ohff, Manuela

“…The bicyclic alcohol (−)- 4 was prepared from (−)-bicyclo[3.2.0]hept-2-en-6-one (−)- 1 in 50% yield. The diol (−)- 4 was coupled to selected chlorophosphines…”
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Synthesis of enantiopure 7-aminobicyclo[3.2.0]hept-2-en-6-ol; a potential N-O chelating ligand for enantioselective catalysis by Dousson, Cyril B., Roberts, Stanley M.

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Discovery of Novel and Potent Thiazoloquinazolines as Selective Aurora A and B Kinase Inhibitors by Jung, Frédéric H, Pasquet, Georges, Lambert-van der Brempt, Christine, Lohmann, Jean-Jacques M, Warin, Nicolas, Renaud, Fabrice, Germain, Hervé, De Savi, Chris, Roberts, Nicola, Johnson, Trevor, Dousson, Cyril, Hill, George B, Mortlock, Andrew A, Heron, Nicola, Wilkinson, Robert W, Wedge, Stephen R, Heaton, Simon P, Odedra, Rajesh, Keen, Nicholas J, Green, Stephen, Brown, Elaine, Thompson, Katherine, Brightwell, Stephen

“…The synthesis of a novel series of quinazolines substituted at C4 by five-membered ring aminoheterocycles is reported. Their in vitro structure−activity…”
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