Publications by authors named "John D Trzupek"

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Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist.
Mark E Schnute, Mattias Wennerstål, Jennifer Alley, Martin Bengtsson, James R Blinn, John D Trzupek

J Med Chem· December 2018

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Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Michael L Vazquez, Neelu Kaila, Joseph W Strohbach, John D Trzupek, Matthew F Brown

J Med Chem· February 2018

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Discovery of Clinical Candidate 1-{[(2S,3S,4S)-3-Ethyl-4-fluoro-5-oxopyrrolidin-2-yl]methoxy}-7-methoxyisoquinoline-6-carboxamide (PF-06650833), a Potent, Selective Inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4), by Fragment-Based Drug Design.
Katherine L Lee, Catherine M Ambler, David R Anderson, Brian P Boscoe, Andrea G Bree, John D Trzupek

J Med Chem· July 2017

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Identification of a Chemical Probe for Family VIII Bromodomains through Optimization of a Fragment Hit.
Brian S Gerstenberger, John D Trzupek, Cynthia Tallant, Oleg Fedorov, Panagis Filippakopoulos

J Med Chem· May 2016

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Reversal of Diastereoselection in the Conjugate Addition of Cuprates to Unsaturated Lactams.
Stephen W Wright, Chulho Choi, Seungwon Chung, Brian P Boscoe, Susan E Drozda, John D Trzupek

Org Lett· November 2015

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Selective targeting of the BRG/PB1 bromodomains impairs embryonic and trophoblast stem cell maintenance.
Oleg Fedorov, Josefina Castex, Cynthia Tallant, Dafydd R Owen, Sarah Martin, John D Trzupek

Sci Adv· November 2015

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Epigenetic drugs that do not target enzyme activity.
Dafydd R Owen, John D Trzupek

Drug Discov Today Technol· June 2014

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Identification of a chemical probe for bromo and extra C-terminal bromodomain inhibition through optimization of a fragment-derived hit.
Paul V Fish, Panagis Filippakopoulos, Gerwyn Bish, Paul E Brennan, Mark E Bunnage, John D Trzupek

J Med Chem· November 2012

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Total synthesis of complestatin: development of a Pd(0)-mediated indole annulation for macrocyclization.
Hiroyuki Shimamura, Steven P Breazzano, Joie Garfunkle, F Scott Kimball, John D Trzupek

J Am Chem Soc· June 2010

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Total synthesis of enantiopure phalarine via a stereospecific Pictet-Spengler reaction: traceless transfer of chirality from L-tryptophan.
John D Trzupek, Dongjoo Lee, Brendan M Crowley, Vasilios M Marathias, Samuel J Danishefsky

J Am Chem Soc· June 2010

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Lessons from the Total Synthesis of (±) Phalarine: Insights Into the Mechanism of the Pictet-Spengler Reaction.
John D Trzupek, Chaomin Li, Collin Chan, Brendan M Crowley, Annekatrin C Heimann

Pure Appl Chem· April 2010

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Total synthesis of chloropeptin II (complestatin) and chloropeptin I.
Joie Garfunkle, F Scott Kimball, John D Trzupek, Shinobu Takizawa, Hiroyuki Shimamura

J Am Chem Soc· November 2009

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Toward homogeneous erythropoietin: chemical synthesis of the Ala1-Gly28 glycopeptide domain by "alanine" ligation.
Cindy Kan, John D Trzupek, Bin Wu, Qian Wan, Gong Chen

J Am Chem Soc· April 2009

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A unique class of duocarmycin and CC-1065 analogues subject to reductive activation.
Wei Jin, John D Trzupek, Thomas J Rayl, Melinda A Broward, George A Vielhauer

J Am Chem Soc· December 2007

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Systematic exploration of the structural features of yatakemycin impacting DNA alkylation and biological activity.
Mark S Tichenor, Karen S MacMillan, John D Trzupek, Thomas J Rayl, Inkyu Hwang

J Am Chem Soc· September 2007

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Asymmetric total synthesis of (+)- and ent-(-)-yatakemycin and duocarmycin SA: evaluation of yatakemycin key partial structures and its unnatural enantiomer.
Mark S Tichenor, John D Trzupek, David B Kastrinsky, Futoshi Shiga, Inkyu Hwang

J Am Chem Soc· December 2006

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Alkylation of duplex DNA in nucleosome core particles by duocarmycin SA and yatakemycin.
John D Trzupek, Joel M Gottesfeld, Dale L Boger

Nat Chem Biol· February 2006

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Photochemical generation of ribose abasic sites in RNA oligonucleotides.
John D Trzupek, Terry L Sheppard

Org Lett· April 2005

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A novel achiral seco-amino-cyclopropylindoline (CI) analog of CC-1065 and the duocarmycins: design, synthesis and biological studies.
James L Toth, John D Trzupek, Lloyd V Flores, Konstantinos Kiakos, John A Hartley

Med Chem· January 2005

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Synthesis and evaluation of N-aryl and N-alkenyl CBI derivatives.
Jay P Parrish, John D Trzupek, Terry V Hughes, Inkyu Hwang, Dale L Boger

Bioorg Med Chem· November 2004

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