Publications scientifiques
Chez Paraza, la science est au premier plan de tout ce que nous faisons. Nous nous consacrons au développement de nouvelles technologies qui feront progresser le domaine de la découverte de médicaments. Nos travaux, qu’il s’agisse de partenariats avec des clients, de collaborations universitaires ou de recherches internes, sont régulièrement publiés dans des revues de premier plan. Explorez nos dernières publications scientifiques pour découvrir comment nos scientifiques contribuent à l’amélioration de la santé humaine, une découverte à la fois.
Jun Liang, Michael J. Lambrecht, Teresita L. Arenzana, Samuel Aubert-Nicol, Linda Bao, Fabio Broccatelli, Jianping Cai, Celine Eidenschenk, Christine Everett, Thomas Garner, Felix Gruber, Pouyan Haghshenas, Malcolm P. Huestis, Peter L. Hsu, Ponien Kou, Araz Jakalian, Robin Larouche-Gauthier, Jean-Philippe Leclerc, Dennis H. Leung, Aaron Martin, Jeremy Murray, Madeleine Prangley, Sascha Rutz, Satoko Kakiuchi-Kiyota, Alexander Lee Satz, Nicholas J. Skelton, Micah Steffek, Daniel Stoffler, Jawahar Sudhamsu, Sophia Tan, Jian Wang, Shouliang Wang, Qiuyue Wang, Timothy J.Wendorff, Moreno Wichert, Arun Yadav, Christine Yu, and Xiaojing Wang. Optimization of a Novel DEL Hit That Binds in the Cbl-b SH2 Domain and Blocks Substrate Binding, ACS Med. Chem. Lett. 2024, ASAP
https://pubs.acs.org/doi/10.1021/acsmedchemlett.4c00068
Marie-Gabrielle Braun, Avi Ashkenazi, Ramsay E. Beveridge, Georgette Castanedo, Heidi Ackerly Wallweber, Maureen H. Beresini, Kevin R. Clark, Tom De Bruyn, Liqiang Fu, Paul Gibbons, Fan Jiang, Susan Kaufman, David Kan, James R. Kiefer, Jean-Philippe Leclerc, Alexandre Lemire, Cuong Ly, Ehud Segal, Jessica Sims, Weiru Wang, Wentao Wei, Liang Zhao, Jacob B. Schwarz, and Joachim Rudolph. Discovery of Potent, Selective, and Orally Available IRE1α Inhibitors Demonstrating Comparable PD Modulation to IRE1 Knockdown in a Multiple Myeloma Model ACS Med. Chem. Lett., 2024, In Press
https://pubs.acs.org/doi/10.1021/acs.jmedchem.3c02425
Audrey Belouin, Guillaume Pelletier, Frederic Vuillermet, Joanick Bourret, Tess Fortier. Activation/Cyclization of 2H-Azirines and 3-Amino-2-fluoropyridines Towards 2-Aryl-Pyrido[2,3-b]pyrazines. Eur. J. Org. Chem. 2024, In Press
https://chemistry-europe.onlinelibrary.wiley.com/doi/10.1002/ejoc.202400297
Samuel A. Fisher, Connor M. Simon, Peter L. Fox, Michael J. Cotnam, Patrick L. DeRoy, and Mark Stradiotto. Thermal Nickel-Catalyzed N-Arylation of NH-Sulfoximines with (Hetero)aryl Chlorides Enabled by PhPAd-DalPhos Ligation Org. Lett. 2024, ASAP
https://pubs.acs.org/doi/10.1021/acs.orglett.3c04152
Jack A. Terrett, Justin Q. Ly, Paula Katavolos, Catrin Hasselgren, Steven Laing, Fiona Zhong, Elisia Villemure, Martin Déry, Robin Larouche-Gauthier, Huifen Chen, Daniel G. Shore, Wyne P. Lee, Eric Suto, Kevin Johnson, Marjory Brooks, Alyssa Stablein, Francis Beaumier, Léa Constantineau-Forget, Chantal Grand-Maître, Luce Lépissier, Stéphane Ciblat, Claudio Sturino, Yong Chen, Baihua Hu, Justin Elstrott, Vineela Gandham, Victory Joseph, Helen Booler, Gary Cain, Carolina Chou, Aaron Fullerton, Michelle Lepherd, Shannon Stainton, Elizabeth Torres, Konnie Urban, Lanlan Yu, Yu Zhong, Linda Bao, Kang-Jye Chou, Jessica Lin, Wei Zhang, Hank La, Liling Liu, Teresa Mulder, Jun Chen, Tania Chernov-Rogan, Adam R. Johnson, David H. Hackos, Rebecca Leahey, Shannon D. Shields, Alessia Balestrini, Lorena Riol-Blanco, Brian S. Safina, Matthew Volgraf, Steven Magnuson, and Satoko Kakiuchi-Kiyota. Discovery of TRPA1 Antagonist GDC-6599: Derisking Preclinical Toxicity and Aldehyde Oxidase Metabolism with a Potential First-In-Class Therapy for Respiratory Disease J. Med. Chem. 2024, 67, 3287.
https://pubs.acs.org/doi/10.1021/acs.jmedchem.3c02121
Amanda Yaneza, and Alexandria D. M. Jeanneret. Synthesis of Heterodiarylmethanes via Metallaphotoredox Decarboxylative Arylation Synlett 2024, ASAP
https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0042-1751550
Alberto dos Santos Pereira. Effect of water and protic solvents on polysaccharide-based column efficiency J. Sep. Sci. 2023, 2300538
https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/10.1002/jssc.202300538
https://analyticalsciencejournals.onlinelibrary.wiley.com/doi/10.1002/jssc.202300538Mingshuo Zeng, Jessica M. Grandner, Marian C. Bryan, Vishal Verma, Robin Larouche-Gauthier, Jean-Philippe Leclerc, Liang Zhao, Pouyan Haghshenas, Samuel Aubert-Nicol, Arun Yadav, Melissa Ashley, Jacob Z. Chen, Matthew Durk, Karen E. Samy, Marika Nespi, Elizabeth Levy, Karl Merrick, John G. Moffat, Jeremy Murray, Angela Oh, Christine Orr, Ehud Segal, Jessica Sims, Christopher Sneeringer, Madeleine Prangley, Steffan Vartanian, Steven Magnuson, and Brendan T. Parr. Discovery of Selective Tertiary Amide Inhibitors of Cyclin-Dependent Kinase 2 (CDK2) ACS Med. Chem. Lett. 2023, 14, 1179
https://doi.org/10.1021/acsmedchemlett.3c00142
Connor M. Simon, Katherine N. Robertson, Patrick L. DeRoy, Arun A. Yadav, Erin R. Johnson, Mark Stradiotto Nickel-Catalyzed N-Arylation of Sulfinamides: A Comparative Study versus Analogous Sulfonamide Cross-Couplings Organometallics 2023, 42, 1704
https://doi.org/10.1021/acs.organomet.2c00545
Wanying Zhang, Juliana Smillovich, Vincent Albert. Palladium Catalyzed Amidation of Phenyl Carboxylates and Anilines Using Aqueous Micellar Catalysis Tet. Lett. 2023, 114, 154242
https://doi.org/10.1016/j.tetlet.2022.154242
Ryan T. McGuire, Travis Lundrigan, Joshua W. M. MacMillan, Katherine N. Robertson, Arun A. Yadav, Mark Stradiotto. Mapping Dual-Base-Enabled Nickel-Catalyzed Aryl Amidations: Application in the Synthesis of 4-Quinolones Angew. Chem. Int. Ed. 2023, 61, e202200352
https://doi.org/10.1002/anie.202200352
Monica Bubenik, Pavel Mader, Philippe Mochirian, Fréderic Vallée, Jillian Clark, Jean-François Truchon, Alexander L. Perryman, Victor Pau, Igor Kurinov, Karl E. Zahn, Marie-Eve Leclaire, Robert Papp, Marie-Claude Mathieu, Martine Hamel, Nicole M. Duffy, Claude Godbout, Matias Casas-Selves, Jean-Pierre Falgueyret, Prasamit S. Baruah, Olivier Nicolas, Rino Stocco, Hugo Poirier, Giovanni Martino, Alexanne Bonneau Fortin, Anne Roulston, Amandine Chefson, Stéphane Dorich, Miguel St-Onge, Purvish Patel, Charles Pellerin, Stéphane Ciblat, Thomas Pinter, Francis Barabé, Majida El Bakkouri, Paranjay Parikh, Christian Gervais, Agnel Sfeir, Yael Mamane, Stephen J. Morris, W. Cameron Black, Frank Sicheri, Michel Gallant. Identification of RP-6685, an Orally Bioavailable Compound that Inhibits the DNA Polymerase Activity of Polθ J. Med. Chem. 2022, 65, 13198
https://doi.org/10.1021/acs.jmedchem.2c00998
Sanju Narayanan, Doughua Dai, Ravi Kumar Vyas Devambatla, Vincent Albert, Nicolas Bruneau-Latour, Vineetha Vasukuttan, Stephane Ciblat, Kenneth Rehder, Scott P. Runyon, Rangan Maitra. Synthesis and Characterization of an Orally Bioavailable Small Molecule Agonist of the Apelin Receptor Bioorg. Med. Chem. 2022, 66, 116789
https://doi.org/10.1016/j.bmc.2022.116789
Jason J. Marineau, Kristin B. Hamman, Shanhu Hu, Sydney Alnemy, Janessa Mihalich, Anzhelika Kabro, Kenneth Matthew Whitmore, Dana K. Winter, Stephanie Roy, Stephane Ciblat, Nan Ke, Anneli Savinainen, Ashraf Wilsily, Goran Malojcic, Robert Zahler, Darby Schmidt, Michael J. Bradley, Nigel J. Waters, Claudio Chuaqui. Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7 J. Med. Chem. 2022, 65, 1458
https://doi.org/10.1021/acs.jmedchem.1c01171
Frédéric Vuillermet, Joanick Bourret, Guillaume Pelletier. Synthesis of Imidazo[1,2‑a]pyridines: Triflic Anhydride-Mediated Annulation of 2H‑Azirines with 2‑Chloropyridines J. Org. Chem. 2021, 86, 388
https://doi.org/10.1021/acs.joc.0c02148
Elisia Villemure, Jack A. Terrett, Robin Larouche-Gauthier, Martin Déry, Huifen Chen, Rebecca M. Reese, Shannon D. Shields, Jun Chen, Steven Magnuson, Matthew Volgraf. A Retrospective Look at the Impact of Binding Site Environment on the Optimization of TRPA1 Antagonists ACS Med. Chem. Lett. 2021, 12, 1230
https://doi.org/10.1021/acsmedchemlett.1c00305
Jack A. Terrett, Huifen Chen, Daniel G. Shore, Elisia Villemure, Robin Larouche-Gauthier, Martin Déry, Francis Beaumier, Léa Constantineau-Forget, Chantal Grand-Maître, Luce Lépissier, Stéphane Ciblat, Claudio Sturino, Yong Chen, Baihua Hu, Aijun Lu, Yunli Wang, Andrew P. Cridland, Stuart I. Ward, David H. Hackos, Rebecca M. Reese, Shannon D. Shields, Jun Chen, Alessia Balestrini, Lorena Riol-Blanco, Wyne P. Lee, John Liu, Eric Suto, Xiumin Wu, Juan Zhang, Justin Q. Ly, Hank La, Kevin Johnson, Matt Baumgardner, Kang-Jye Chou, Alexis Rohou, Lionel Rougé, Brian S. Safina, Steven Magnuson, Matthew Volgraf. Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy J. Med. Chem. 2021, 64, 3843
https://doi.org/10.1021/acs.jmedchem.0c02023
Malcolm P. Huestis, Jean-Philippe Leclerc, Robin Larouche-Gauthier, Samuel Aubert-Nicol, Arun Yadav, Koilpitchai Sivamuthuraman. Cp*Rh(III)-Catalyzed C8 C−H Alkylation of Quinoline N-Oxides with Diazo Meldrum’s Acid Eur. J. Org. Chem. 2021, 396
https://doi.org/10.1002/ejoc.202001584
Ramsay E. Beveridge, Heidi Ackerly Wallweber, Avi Ashkenazi, Maureen Beresini, Kevin R. Clark, Paul Gibbons, Élise Ghiro, Susan Kaufman, Alexandre Larivée, Mélissa Leblanc, Jean-Philippe Leclerc, Alexandre Lemire, Cuong Ly, Joachim Rudolph, Jacob B. Schwarz, Sanjay Srivastava, Weiru Wang, Liang Zhao, Marie-Gabrielle Braun. Identification of BRaf-Sparing Amino-Thienopyrimidines with Potent IREa Inhibitory Activity ACS Med. Chem. Lett. 2020, 11, 2389
https://doi.org/10.1021/acsmedchemlett.0c00344
Jenna K. Rimel, Zachary C. Poss, Benjamin Erickso, Zachary L. Maas, Christopher C. Ebmeier, Jared L. Johnson, Tim-Michael Decker, Tomer M. Yaron, Michael J. Bradley, Kristin B. Hamman, Shanhu Hu, Goran Malojcic, Jason J. Marineau, Peter W. White, Martine Brault, Limei Tao, Patrick DeRoy, Christian Clavette, Shraddha Nayak, Leah J. Damon, Ines H. Kaltheuner, Heeyoun Bunch, Lewis C. Cantley, Matthias Geyer, Janet Iwasa, Robin D. Dowell, David L. Bentley, William M. Old, Dylan J. Taatjes. Selective Inhibition of CDK7 Reveals High-Confidence Targets and New Models for TFIIH Function in Transcription Genes & Dev. 2020, 34, 1452
http://www.genesdev.org/cgi/doi/10.1101/gad.341545.120
Audrey Picard , Stéphane Ciblat , Yeeman K. Ramtohul. Synthesis of α,α-Disubstituted Benzocyclobutane Amino Acids Through [2+2] Annulation of Benzyne with Dehydroalanine Synlett 2020, 31, 507
https://www.thieme-connect.de/products/ejournals/abstract/10.1055/s-0039-1691572
Abhijit Bhat, Stephane Ciblat, Hong Wang, Kollol Pal. The Development of Tropomyosin Receptor Kinase (Trk) Inhibitors as Targeted Cancer Therapeutics Med. Chem. Rev. 2020, 55, 303
Sarah M. Bronner, Karl A. Merrick, Jeremy Murray, Laurent Salphati, John G. Moffat, Jodie Pang, Christopher J. Sneeringer, Nicholas Dompe, Patrick Cyr, Hans Purkey, Gladys de Leon Boenig, Jun Li, Aleksandr Kolesnikov, Robin Larouche-Gauthier, Kwong Wah Lai, Xiaoli Shen, Samuel Aubert-Nicol, Yi-Chen Chen, Jonathan Cheong, James J. Crawford, Marc Hafner, Pouyan Haghshenas, Araz Jakalian, Jean-Philippe Leclerc, Ngiap-Kie Lim, Tom O’Brien, Emile G. Plise, Hadil Shalan, Claudio Sturino, John Wai, Yang Xiao, Jianping Yin, Liang Zhao, Stephen Gould, Alan Olivero, Timothy P. Heffron. Design of a Brain-Penetrant CDK4/6 Inhibitor for Glioblastoma Bioorg. Med. Chem. Lett. 2019, 29, 2294
https://doi.org/10.1016/j.bmcl.2019.06.021
Shanhu Hu, Jason J. Marineau, Nisha Rajagopal, Kristin B. Hamman, Yoon Jong Choi, Darby R. Schmidt, Nan Ke, Liv Johannessen, Michael J. Bradley, David A. Orlando, Sydney R. Alnemy, Yixuan Ren, Stéphane Ciblat, Dana K. Winter, Anzhelika Kabro, Kevin T. Sprott, J. Graeme Hodgson, Christian C. Fritz, John P. Carulli, Emmanuelle di Tomaso, Eric R. Olson. Discovery and Characterization of SY-1365, a Selective, Covalent Inhibitor of CDK7 Cancer Res. 2019, 79, 3479
Alan B. Cooper, Stéphane Ciblat, Gerald Shipps, Jedd Levine, Matthew Kostura, Vibha Oza, Léa Constantineau-Forget, Martin Déry, Chantal Grand-Maître, Nicolas Bruneau-Latour, Édith Bellavance, Michael Patane, Arshad Siddiqui, Michael Luther. 1-Thiazol-2-yl-N-3-methyl-1H-pyrozole-5-carboxylic acid derivatives as antitumor agents Bioorg. Med. Chem. Lett. 2017, 27, 4471
https://doi.org/10.1016/j.bmcl.2017.08.003
Tabinda Ahmad, Julien Dansereau, Martin Hébert, Chantal Grand-Maître, Alexandre Larivée, Arshad Siddiqui, Alexandre Gagnon. Preparation of 3-O-aryl chloramphenicol derivatives via chemoselective copper-catalyzed O-arylation of (1R,2R)-(−)-N-BOC-2-amino-1-(4-nitrophenyl)-1,3-propanediol using triarylbismuthines Tet. Lett. 2016, 57, 4284
https://doi.org/10.1016/j.tetlet.2016.08.021
Hui Ding, Patrick L. DeRoy, Christian Perreault, Alexandre Larivée, Arshad Siddiqui, Charles G. Caldwell, Susan Harran, Patrick G. Harran. Electrolytic Macrocyclizations: Scalable Synthesis of a Diazonamide-Based Drug Development Candidate Angew. Chem. Int. Ed. 2015, 54, 4818
https://doi.org/10.1002/anie.201411663
