Search Results - "FADER, Lee D"

Assessing Atropisomer Axial Chirality in Drug Discovery and Development by LaPlante, Steven R, D. Fader, Lee, Fandrick, Keith R, Fandrick, Daniel R, Hucke, Oliver, Kemper, Ray, Miller, Stephen P. F, Edwards, Paul J

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Revealing Atropisomer Axial Chirality in Drug Discovery by LaPlante, Steven R., Edwards, Paul J., Fader, Lee D., Jakalian, Araz, Hucke, Oliver

“…An often overlooked source of chirality is atropisomerism, which results from slow rotation along a bond axis due to steric hindrance and/or electronic…”
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Preclinical Profile of BI 224436, a Novel HIV-1 Non-Catalytic-Site Integrase Inhibitor by FENWICK, Craig, AMAD, Ma'an, FADER, Lee D, FAUCHER, Anne-Marie, GARNEAU, Michel, JAKALIAN, Araz, KAWAI, Stephen, LAMORTE, Louie, LAPLANTE, Steven, LAIBIN LUO, MASON, Steve, POUPART, Marc-André, BAILEY, Murray D, RIOUX, Nathalie, SCHROEDER, Patricia, SIMONEAU, Bruno, TREMBLAY, Sonia, TSANTRIZOS, Youla, WITVROUW, Myriam, YOAKIM, Christiane, BETHELL, Richard, BÖS, Michael, BONNEAU, Pierre, CORDINGLEY, Michael, COULOMBE, René, DUAN, Jianmin, EDWARDS, Paul

“…BI 224436 is an HIV-1 integrase inhibitor with effective antiviral activity that acts through a mechanism that is distinct from that of integrase strand…”
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Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV‑1 by Fader, Lee D, Malenfant, Eric, Parisien, Mathieu, Carson, Rebekah, Bilodeau, François, Landry, Serge, Pesant, Marc, Brochu, Christian, Morin, Sébastien, Chabot, Catherine, Halmos, Ted, Bousquet, Yves, Bailey, Murray D, Kawai, Stephen H, Coulombe, René, LaPlante, Steven, Jakalian, Araz, Bhardwaj, Punit K, Wernic, Dominik, Schroeder, Patricia, Amad, Ma’an, Edwards, Paul, Garneau, Michel, Duan, Jianmin, Cordingley, Michael, Bethell, Richard, Mason, Stephen W, Bös, Michael, Bonneau, Pierre, Poupart, Marc-André, Faucher, Anne-Marie, Simoneau, Bruno, Fenwick, Craig, Yoakim, Christiane, Tsantrizos, Youla

“…An assay recapitulating the 3′ processing activity of HIV-1 integrase (IN) was used to screen the Boehringer Ingelheim compound collection. Hit-to-lead and…”
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Discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly by Fader, Lee D., Bethell, Richard, Bonneau, Pierre, Bös, Michael, Bousquet, Yves, Cordingley, Michael G., Coulombe, René, Deroy, Patrick, Faucher, Anne-Marie, Gagnon, Alexandre, Goudreau, Nathalie, Grand-Maître, Chantal, Guse, Ingrid, Hucke, Oliver, Kawai, Stephen H., Lacoste, Jean-Eric, Landry, Serge, Lemke, Christopher T., Malenfant, Eric, Mason, Stephen, Morin, Sébastien, O’Meara, Jeff, Simoneau, Bruno, Titolo, Steve, Yoakim, Christiane

“…The discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly is described. Synthesis of analogs of the…”
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Total Synthesis of Bafilomycin A1 by Kleinbeck, Florian, Fettes, Gabriela J., Fader, Lee D., Carreira, Erick M.

“…A convergent synthesis of bafilomycin A1, a potent inhibitor of V‐type ATPases, is presented. The synthesis relies on the zinc triflate mediated…”
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Stereochemically Rich Pentaketides from Bis(isoxazolines):  A General Strategy for Efficient Polyketide Synthesis by Fader, Lee D, Carreira, Erick M

“…A strategy based on diastereoselective dipolar cycloaddition reaction of nitrile oxides and allylic alcoholates has been applied to the synthesis of…”
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Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV by Fader, Lee D, Carson, Rebekah, Morin, Sébastien, Bilodeau, François, Chabot, Catherine, Halmos, Ted, Bailey, Murray D, Kawai, Stephen H, Coulombe, René, Laplante, Steven, Mekhssian, Kevork, Jakalian, Araz, Garneau, Michel, Duan, Jianmin, Mason, Stephen W, Simoneau, Bruno, Fenwick, Craig, Tsantrizos, Youla, Yoakim, Christiane

“…A scaffold replacement approach was used to identifying the pyridine series of noncatalytic site integrase inhibitors. These molecules bind with higher…”
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RP-3500: A Novel, Potent, and Selective ATR Inhibitor that is Effective in Preclinical Models as a Monotherapy and in Combination with PARP Inhibitors by Roulston, Anne, Zimmermann, Michal, Papp, Robert, Skeldon, Alexander, Pellerin, Charles, Dumas-Bérube, Émilie, Dumais, Valerie, Dorich, Stéphane, Fader, Lee D, Fournier, Sara, Li, Li, Leclaire, Marie-Eve, Yin, Shou Yun, Chefson, Amandine, Alam, Hunain, Yang, William, Fugère-Desjardins, Chloe, Vignini-Hammond, Sabrina, Skorey, Kathryn, Mulani, Amina, Rimkunas, Victoria, Veloso, Artur, Hamel, Martine, Stocco, Rino, Mamane, Yael, Li, Zuomei, Young, Jordan T F, Zinda, Michael, Black, W Cameron

“…Ataxia telangiectasia and Rad3-related (ATR) kinase protects genome integrity during DNA replication. RP-3500 is a novel, orally bioavailable clinical-stage…”
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Discovery of the Potent and Selective ATR Inhibitor Camonsertib (RP-3500) by Black, W. Cameron, Abdoli, Abbas, An, Xiuli, Auger, Anick, Beaulieu, Patrick, Bernatchez, Michel, Caron, Cathy, Chefson, Amandine, Crane, Sheldon, Diallo, Mohamed, Dorich, Stéphane, Fader, Lee D., Ferraro, Gino B., Fournier, Sara, Gao, Qi, Ginzburg, Yelena, Hamel, Martine, Han, Yongshuai, Jones, Paul, Lanoix, Stéphanie, Lacbay, Cyrus M., Leclaire, Marie-Eve, Levy, Maayan, Mamane, Yael, Mulani, Amina, Papp, Robert, Pellerin, Charles, Picard, Audrey, Skeldon, Alexander, Skorey, Kathryn, Stocco, Rino, St.-Onge, Miguel, Truchon, Jean-François, Truong, Vouy Linh, Zimmermann, Michal, Zinda, Michael, Roulston, Anne

“…ATR is a key kinase in the DNA-damage response (DDR) that is synthetic lethal with several other DDR proteins, making it an attractive target for the treatment…”
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Discovery of NXT-10796, an orally active, intestinally restricted EP4 agonist prodrug for the treatment of inflammatory bowel disease by St.-Onge, Miguel, Chefson, Amandine, Wu, Joyce, Caron-Duval, Édouard, Dumais, Valerie, Dorich, Stephane, Cox, Jennifer, Caron, Alex, Burch, Jason, Percival, M. David, Therien, Alex G., Fader, Lee D.

“…[Display omitted] A property-focused optimization strategy was employed to modify the carboxylic acid head group of a class of EP4 agonists in order to…”
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Novel pyridone EP4 agonists featuring allylic alcohol ω-chains by Dorich, Stéphane, Cox, Jennifer H., Burch, Jason D., Chagnon, Félix, Chen, Bin, Léger, Serge, St-Onge, Miguel, Fader, Lee D.

“…[Display omitted] Novel prostaglandin E2 receptor 4 (EP4) agonists featuring a pyridone core and an allylic alcohol ω-chain were discovered. These agonists…”
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Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 1: Addressing configurational instability through scaffold modification by Fader, Lee D., Landry, Serge, Morin, Sébastien, Kawai, Stephen H., Bousquet, Yves, Hucke, Oliver, Goudreau, Nathalie, Lemke, Christopher T., Bonneau, Pierre, Titolo, Steve, Mason, Stephen, Simoneau, Bruno

“…The optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly that possess a labile stereocenter at C3 is…”
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Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 2: Structure–activity relationships (SAR) of the C3-phenyl moiety by Fader, Lee D., Landry, Serge, Goulet, Sylvie, Morin, Sébastien, Kawai, Stephen H., Bousquet, Yves, Dion, Isabelle, Hucke, Oliver, Goudreau, Nathalie, Lemke, Christopher T., Rancourt, Jean, Bonneau, Pierre, Titolo, Steve, Amad, Ma’an, Garneau, Michel, Duan, Jianmin, Mason, Stephen, Simoneau, Bruno

“…Detailed structure–activity relationships of the C3-phenyl moiety that allow for the optimization of antiviral potency of a series of…”
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Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs by Fader, Lee D, Bailey, Murray, Beaulieu, Eric, Bilodeau, François, Bonneau, Pierre, Bousquet, Yves, Carson, Rebekah J, Chabot, Catherine, Coulombe, René, Duan, Jianmin, Fenwick, Craig, Garneau, Michel, Halmos, Ted, Jakalian, Araz, James, Clint, Kawai, Stephen H, Landry, Serge, LaPlante, Steven R, Mason, Stephen W, Morin, Sebastien, Rioux, Nathalie, Simoneau, Bruno, Surprenant, Simon, Thavonekham, Bounkham, Thibeault, Carl, Trinh, Thao, Tsantrizos, Youla, Tsoung, Jennifer, Yoakim, Christiane, Wernic, Dominik

“…Optimization of pyridine-based noncatalytic site integrase inhibitors (NCINIs) based on compound 2 has led to the discovery of molecules capable of inhibiting…”
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Cover Picture: Revealing Atropisomer Axial Chirality in Drug Discovery (ChemMedChem 3/2011) by LaPlante, Steven R., Edwards, Paul J., Fader, Lee D., Jakalian, Araz, Hucke, Oliver

“…The cover picture shows that an atropisomeric drug dosed as a single enantiomer can racemize as a result of axial rotation along a hindered bond…”
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Synthesis of novel analogs of aromatic peptide nucleic acids (APNAs) with modified conformational and electrostatic properties by Fader, Lee D, Myers, Eddie L, Tsantrizos, Youla S

“…Aromatic peptide nucleic acid analogs having an N-(2-aminobenzyl)glycine backbone (APNA 1 ) were previously identified as promising new leads for the design of…”
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Hybridization Properties of Aromatic Peptide Nucleic Acids:  A Novel Class of Oligonucleotide Analogues by Fader, Lee D, Tsantrizos, Youla S

“…The synthesis of APNA-PNA chimeras containing all four DNA bases will be described. The hybridization properties of APNA-PNA chimeras with DNA and RNA are…”
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Discovery of Potent and Orally Bioavailable Pyrimidine Amide cGAS Inhibitors via Structure-Guided Hybridization by Cyr, Patrick, Fader, Lee D., Burch, Jason D., Pike, Kelly A., Sietsema, Daniel V., Boily, Marc-Olivier, Ciblat, Stéphane, Sgarioto, Nicolas, Skeldon, Alexander M., Gaudreault, Samuel, Le Gros, Philippe, Dumais, Valérie, McKay, Daniel J. J., Abraham, Nathan S., Seliniotakis, Ria, Beveridge, Ramsay E.

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Total Synthesis of Bafilomycin A 1 by Kleinbeck, Florian, Fettes, Gabriela J., Fader, Lee D., Carreira, Erick M.

“…A convergent synthesis of bafilomycin A 1 , a potent inhibitor of V‐type ATPases, is presented. The synthesis relies on the zinc triflate mediated…”
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