Structural and Physicochemical Features of Oral PROTACs
Schade, Markus, Scott, James S., Hayhow, Thomas G., Pike, Andy, Terstiege, Ina, Ahlqvist, Marie, Johansson, Johan R., Diene, Coura R., Fallan, Charlene, Balazs, Amber Y. S., Chiarparin, Elisabetta, Wilson, David
Published in Journal of medicinal chemistry (08.08.2024)
Published in Journal of medicinal chemistry (08.08.2024)
Get full text
Journal Article
A Buchwald–Hartwig Protocol to Enable Rapid Linker Exploration of Cereblon E3‐Ligase PROTACs
Hayhow, Thomas G., Borrows, Rachel E. A., Diène, Coura R., Fairley, Gary, Fallan, Charlene, Fillery, Shaun M., Scott, James S., Watson, David W.
Published in Chemistry : a European journal (15.12.2020)
Published in Chemistry : a European journal (15.12.2020)
Get full text
Journal Article
Synthesis of (4 ' R)-Azido-(2 ' R)-2 '-Deoxy-2 '-C-Methyluridine and Its Esters by Direct Iodide Displacement
Benhaim, Cyril, Lemaire, Sebastien, Gaekens, Tim, Govaerts, Tom, Houpis, Iaonnis N., Reniers, Peter, Van Looy, Anja, Vermeulen, Wim A. A., Bernhardt, Sebastian, Diene, Coura, Knochel, Paul, Farina, Vittorio
Published in Synlett (12.08.2013)
Published in Synlett (12.08.2013)
Get more information
Journal Article
The Role of Intramolecular Reactions and Chemical Degradation in the Apparent Biotransformation Pathways of a Series of SYK Inhibitors
Calle, Beatriz, Barlaam, Bernard, Diène, Coura, Lenz, Eva, Martin, Scott, Sarkar, Ujjal, Wilkinson, Stephen, Pike, Andy
Published in Drug metabolism and disposition (17.06.2024)
Published in Drug metabolism and disposition (17.06.2024)
Get full text
Journal Article
Access to a Diverse Array of Bridged Benzo[1,5]oxazocine and Benzo[1,4]diazepine Structures
Sherborne, Grant J., Diene, Coura, Kemmitt, Paul, Smith, Andrew D.
Published in Organic letters (08.12.2023)
Published in Organic letters (08.12.2023)
Get full text
Journal Article
Discovery of a Series of Orally Bioavailable Androgen Receptor Degraders for the Treatment of Prostate Cancer
Bagal, Sharan K., Astles, Peter C., Diène, Coura, Argyrou, Argyrides, Crafter, Claire, Cassar, Doyle J., Fallan, Charlene, Hock, Andreas, Jones, Thomas, Moreau, Kevin, Lamont, Gillian M., Lamont, Scott, Michaloglou, Chrysiis, Packer, Martin J., Pike, Andy, Ramos-Montoya, Antonio, Scott, James S., Shaw, Joseph, Shologu, Ziyanda
Published in Journal of medicinal chemistry (25.07.2024)
Published in Journal of medicinal chemistry (25.07.2024)
Get full text
Journal Article
Stereoselective C-Glycosylation Reactions with Arylzinc Reagents
Lemaire, Sébastien, Houpis, Ioannis N, Xiao, Tingting, Li, Juanjuan, Digard, Eric, Gozlan, Charlotte, Liu, Renmao, Gavryushin, Andrey, Diène, Coura, Wang, Youchu, Farina, Vittorio, Knochel, Paul
Published in Organic letters (16.03.2012)
Published in Organic letters (16.03.2012)
Get full text
Journal Article
Optimization of Pan-Pim Kinase Activity and Oral Bioavailability Leading to Diaminopyrazole (GDC-0339) for the Treatment of Multiple Myeloma
Wang, Xiaojing, Blackaby, Wesley, Allen, Vivienne, Chan, Grace Ka Yan, Chang, Jae H, Chiang, Po-Chang, Diène, Coura, Drummond, Jason, Do, Steven, Fan, Eric, Harstad, Eric B, Hodges, Alastair, Hu, Huiyong, Jia, Wei, Kofie, William, Kolesnikov, Aleksandr, Lyssikatos, Joseph P, Ly, Justin, Matteucci, Mizio, Moffat, John G, Munugalavadla, Veerendra, Murray, Jeremy, Nash, David, Noland, Cameron L, Del Rosario, Geoff, Ross, Leanne, Rouse, Craig, Sharpe, Andrew, Slaga, Dionysos, Sun, Minghua, Tsui, Vickie, Wallweber, Heidi, Yu, Shang-Fan, Ebens, Allen J
Published in Journal of medicinal chemistry (28.02.2019)
Published in Journal of medicinal chemistry (28.02.2019)
Get full text
Journal Article
Preparation of 2′-Deoxy-2′-spirocyclopropylcytidine via an Alternative Cyclopropanation Reaction
Lemaire, Sébastien, Diène, Coura, Gavryushin, Andrei, Du Jourdin, Xavier Mollat, Paolini, Léa, Jusseau, Xavier, Knochel, Paul, Farina, Vittorio
Published in Journal of organic chemistry (19.04.2019)
Published in Journal of organic chemistry (19.04.2019)
Get full text
Journal Article
Identification and optimisation of a pyrimidopyridone series of IRAK4 inhibitors
Cumming, Iain A., Degorce, Sébastien L., Aagaard, Anna, Braybrooke, Erin L., Davies, Nichola L., Diène, Coura R., Eatherton, Andrew J., Felstead, Hannah R., Groombridge, Sam D., Lenz, Eva M., Li, Yunxia, Nai, Youfeng, Pearson, Stuart, Robb, Graeme R., Scott, James S., Steward, Oliver R., Wu, Chengyan, Xue, Yafeng, Zhang, Lanping, Zhang, Yanxiu
Published in Bioorganic & medicinal chemistry (01.06.2022)
Published in Bioorganic & medicinal chemistry (01.06.2022)
Get full text
Journal Article
Improving metabolic stability and removing aldehyde oxidase liability in a 5-azaquinazoline series of IRAK4 inhibitors
Degorce, Sébastien L., Aagaard, Anna, Anjum, Rana, Cumming, Iain A., Diène, Coura R., Fallan, Charlene, Johnson, Tony, Leuchowius, Karl-Johan, Orton, Alexandra L., Pearson, Stuart, Robb, Graeme R., Rosen, Alan, Scarfe, Graeme B., Scott, James S., Smith, James M., Steward, Oliver R., Terstiege, Ina, Tucker, Michael J., Turner, Paul, Wilkinson, Stephen D., Wrigley, Gail L., Xue, Yafeng
Published in Bioorganic & medicinal chemistry (01.12.2020)
Published in Bioorganic & medicinal chemistry (01.12.2020)
Get full text
Journal Article
Isoxazole-Embedded Allylic Zinc Reagent for the Diastereoselective Preparation of Highly Functionalized Aldol-Type Derivatives Bearing a Stereocontrolled Quaternary Center
Klier, Lydia, Diène, Coura R., Schickinger, Manuel, Metzger, Albrecht, Wagner, Andreas J., Karaghiosoff, Konstantin, Marek, Ilan, Knochel, Paul
Published in Chemistry : a European journal (20.10.2014)
Published in Chemistry : a European journal (20.10.2014)
Get full text
Journal Article
Preparation of Polyfunctional Zinc Organometallics Using an Fe- or Co-Catalyzed Cl/Zn-Exchange
Melzig, Laurin, Diène, Coura R, Rohbogner, Christoph J, Knochel, Paul
Published in Organic letters (17.06.2011)
Published in Organic letters (17.06.2011)
Get full text
Journal Article
Preparation of functionalized Zn and Mg-organometallics. Application to the performance of diastereoselective cross-couplings
Get full text
Journal Article
Conference Proceeding
Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity
Smith, James M., Barlaam, Bernard, Beattie, David, Bradshaw, Lauren, Chan, Ho Man, Chiarparin, Elisabetta, Collingwood, Olga, Cooke, Sophie L., Cronin, Anna, Cumming, Iain, Dean, Emma, Debreczeni, Judit É., del Barco Barrantes, Iván, Diene, Coura, Gianni, Davide, Guerot, Carine, Guo, Xiaoxiao, Guven, Sinem, Hayhow, Thomas G., Hong, Ted, Kemmitt, Paul D., Lamont, Gillian M., Lamont, Scott, Lynch, James T., McWilliams, Lisa, Moore, Shaun, Raubo, Piotr, Robb, Graeme R., Robinson, James, Scott, James S., Srinivasan, Bharath, Steward, Oliver, Stubbs, Christopher J., Syson, Karl, Tan, Lixiang, Turner, Oliver, Underwood, Elizabeth, Urosevic, Jelena, Vazquez-Chantada, Mercedes, Whittaker, Amy L., Wilson, David M., Winter-Holt, Jon J.
Published in Journal of medicinal chemistry (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
Get full text
Journal Article
ChemInform Abstract: Isoxazole-Embedded Allylic Zinc Reagent for the Diastereoselective Preparation of Highly Functionalized Aldol-Type Derivatives Bearing a Stereocontrolled Quaternary Center
Klier, Lydia, Diene, Coura R., Schickinger, Manuel, Metzger, Albrecht, Wagner, Andreas J., Karaghiosoff, Konstantin, Marek, Ilan, Knochel, Paul
Published in ChemInform (01.04.2015)
Published in ChemInform (01.04.2015)
Get full text
Journal Article
Metabolism-driven in vitro/in vivo disconnect of an oral ERɑ VHL-PROTAC
Hayhow, Thomas G, Williamson, Beth, Lawson, Mandy, Cureton, Natalie, Braybrooke, Erin L, Campbell, Andrew, Carbajo, Rodrigo J, Cheraghchi-Bashi, Azadeh, Chiarparin, Elisabetta, Diène, Coura R, Fallan, Charlene, Fisher, David I, Goldberg, Frederick W, Hopcroft, Lorna, Hopcroft, Philip, Jackson, Anne, Kettle, Jason G, Klinowska, Teresa, Künzel, Ulrike, Lamont, Gillian, Lewis, Hilary J, Maglennon, Gareth, Martin, Scott, Gutierrez, Pablo Morentin, Morrow, Christopher J, Nikolaou, Myria, Nissink, J Willem M, O'Shea, Patrick, Polanski, Radoslaw, Schade, Markus, Scott, James S, Smith, Aaron, Weber, Judith, Wilson, Joanne, Yang, Bin, Crafter, Claire
Published in Communications biology (13.05.2024)
Published in Communications biology (13.05.2024)
Get full text
Journal Article
에스트로겐 수용체 분해 PROTAC
DIENE COURA, SCOTT JAMES STEWART, FALLAN CHARLENE, NISSINK JOHANNES WILHELMUS MARIA, HAYHOW THOMAS GEORGE CHRISTOPHER, YANG BIN, BARLAAM BERNARD CHRISTOPHE
Year of Publication 06.12.2021
Get full text
Year of Publication 06.12.2021
Patent