All Publications

Synthesis of Medium-Bridged Twisted Lactams via Cation–pi Control of the Regiochemistry of the Intramolecular Schmidt Reaction
Michal Szostak, Lei Yao, and Jeffrey Aubé
Journal of Organic Chemistry, 2010, 75, 1235–1243
Proximity Effects in Nucleophilic Addition Reactions to Medium-Bridged Twisted Lactams: Remarkably Stable Tetrahedral Intermediates
Michal Szostak, Lei Yao, and Jeffrey Aubé
Journal of the American Chemical Society, 2010, 132, 2078–2084
Synthesis, Structural Analysis, and Reactivity of Bridged Orthoamides by Intramolecular Schmidt Reaction
Michal Szostak and Jeffrey Aubé
Journal of the American Chemical Society, 2010, 132, 2530–2531
Combinatorial Chemistry and Multiple Parallel Synthesis
Lester A. Mitscher, Jeffrey Aubé, Apurba Dutta, and Jennifer E. Golden
In Burger’s Medicinal Chemistry, 2010, 1-94
Reaction Discovery Using Microfluidic-Based Multidimensional Screening of Polycyclic Iminium Ethers
Jennifer L. Treece, John R. Goodell, David Vander Velde, John A. Porco, Jr., and Jeffrey Aubé
Journal of Organic Chemistry, 2010, 75, 2028–2038
A Tandem Prins/Schmidt Reaction Approach to Marine Alkaloids: Formal and Total Syntheses of Lepadiformines A and C
Angelica M. Meyer, Christopher E. Katz, Sze-Wan Li, David Vander Velde, and Jeffrey Aubé
Organic Letters, 2010, 12, 1244–1247
N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: a Novel Class of Selective, Nonbasic, Nitrogen-Containing -Opioid Receptor Ligands
Kevin J. Frankowski, Partha Ghosh, Vincent Setola, Thuy B Tran, Bryan L. Roth, and Jeffrey Aubé
ACS Medicinal Chemistry Letters, 2010, 1, 189–193
Structural Characterization of N-Protonated Amides. Regioselective N-Activation of Medium-Bridged Twisted Lactams
Michal Szostak, Lei Yao, Victor W. Day, Douglas R. Powell, and Jeffrey Aubé
Journal of the American Chemical Society, 2010, 132, 8836–8837
1,3-Allylic Strain as a Strategic Diversification Element For Constructing Libraries of Substituted 2-Arylpiperidines
Thomas C. Coombs, Gerald H. Lushington, Justin Douglas, and Jeffrey Aubé
Angewandte Chemie, International Edition, 2011, 50, 2734–2737
Synthesis and Receptor Profiling of Stemona Alkaloid Analogs Reveal a Potent Class of Sigma Ligands
Kevin J. Frankowski, Vincent Setola, Jon Evans, Ben Neuenswander, Bryan L. Roth, and Jeffrey Aubé
Proceedings of the National Academy of Sciences (USA), 2011, 108, 6727–6732
Modular Synthesis of Triazole-containing Tri-aryl Alpha Helix Mimetics
Modular Synthesis of Triazole-containing Tri-aryl Alpha Helix Mimetics
European Journal of Organic Chemistry, 2011, 2421-2435
Stereoselectivity in Nucleophilic Additions to 3-Azidoalkanals
Chan Woo Huh, Chad Schroeder, Gurpreet Singh, and Jeffrey Aubé
Journal of Organic Chemistry, 2011, 76, 3160-3165
Medium-bridged Lactams: A New Class of Non-planar Amides
Michal Szostak and Jeffrey Aubé
Organic and Biomolecular Chemistry, 2011, 9, 27–35
Resolution of Carboxylic Acids Using Copper (I)-Promoted Removal of Propargylic Esters Under Neutral Conditions
Partha Ghosh and Jeffrey Aubé
Partha Ghosh and Jeffrey Aubé
Use of a Tandem Prins/Friedel-Crafts Reaction in the Construction of the Indeno-Tetrahydropyridine Core of the Haouamine Alkaloids: Formal Synthesis of (–)-Haouamine A
Erik Fenster, Charlie Fehl, and Jeffrey Aubé
Organic Letters, 2011, 13, 2614–2617
In Situ Generation and Intramolecular Schmidt Reaction of Keto Azides in a Microwave-Assisted Flow Format
Thomas O. Painter, Paul D. Thornton, Mario Orestano, Conrad Santini, Michael G. Organ, and Jeffrey Aubé
Chemistry–A European Journal, 2011, 17, 9595–9598
Reaction Discovery using Complex Bicyclo[3.2.1]Octanoid- Derived Donor-Acceptor Cyclopropanes
John R. Goodell, Jennifer L. Poole, Aaron B. Beeler, Jeffrey Aubé, and John A. Porco, Jr.
Journal of Organic Chemistry, 2011, 76, 9792–9800
High-throughput Screening Identifies a Bisphenol Inhibitor of SV40 Large T-Antigen ATPase Activity
Sandlin P. Seguin, Carrie W. Evans, Miranda Nebane-Akah, Sara McKellip, Subramaniam Ananthan, Nichole A. Tower, Melinda Sosa, Lynn Rasmussen, E. Lucile White, Brooks E. Maki, Daljit S. Matharu, Jennifer E. Golden, Jeffrey Aubé, Jeffrey L. Brodsky, and James W. Noah
Journal of Biomedical Screening, 2012, 17, 194–203
A New Twist on Amide Solvolysis
Jeffrey Aubé
Angewandte Chemie, International Edition, 2012, 51, 3063–3065
Mechanism of the Acid Promoted Intramolecular Schmidt Reaction. Theoretical Assessment of the Importance of Lone Pair–Cation, Cation–π and Steric Effects in Controlling Regioselectivity
Osvaldo Gutierrez, Jeffrey Aubé, and Dean J. Tantillo
Osvaldo Gutierrez, Jeffrey Aubé, and Dean J. Tantillo
Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy
Kevin J. Frankowski, Michael P. Hedrick, Palak Gosali, Kelin Li, Shenghua Shi, David Whipple, Partha Ghosh, Thomas E. Prisinzano, Frank J. Schoenen, Ying Su, S. Vasile, Eduard Sergienko, Wilson Gray, Santosh Hariharan, Loribelle Milan, Susanne Heynen-Genel, Arianna Mangravita-Novo, Michael Vicchiarelli, Layton H. Smith, John M. Streicher, Marc G. Caron, Lawrence S. Barak, Laura M. Bohn, Thomas D.Y. Chung and Jeffrey Aubé
ACS Chemical Neuroscience, 2012, 3, 221–236
Drug Repurposing and the Medicinal Chemist
Jeffrey Aubé
ACS Medicinal Chemistry Letters, 2012, 3, 442-444
Principles of Asymmetric Synthesis 2nd Edition
Robert E. Gawley and Jeffrey Aubé
Elsevier: Oxford, 2012, 555 pp

The Schmidt Reaction
Aaron Wrobleski, Thomas C. Coombs, Chan Woo Huh, Sze-Wan Li, and Jeffrey Aubé
Organic Reactions, 2012, 78, 1-320
Natural Products Inspire a New Approach To Oligomer Libraries
Jeffrey Aubé
Nature Chemistry, 2012, 4, 71-72
Identification of a Small Molecule Yeast TORC1 Inhibitor with a Flow Cytometry-Based Multiplex Screen
Jun Chen, Susan M. Young, Chris Allen, Andrew Seeber, Marie-Pierre Péli-Gulli, Nicolas Panchaud, Anna Waller, Oleg Ursu, Tuanli Yao, Jennifer E. Golden, J. Jacob, Strouse, Mark B. Carter, Huining Kang, Cristian G. Bologa, Terry D. Foutz, Bruce S. Edwards, Blake R. Peterson, Jeffrey Aubé, Margaret Werner-Washburne, Robbie J. Loewith, Claudio De Virgilio, and Larry A. Sklar
ACS Chemical Biology, 2012, 7, 715–722
Optimization of Potent Hepatitis C Virus NS3 Helicase Inhibitors Isolated from the Yellow Dyes Thioflavine S and Primuline
Kelin Li, Kevin Frankowski, Craig Belon, Benjamin Neunswander, Jean Ndjomou, Alicia Hanson, Matthew Shanahan, Frank Schoenen, Brian Blagg, Jeffrey Aubé, and David Frick
Journal of Medicinal Chemistry, 2012, 55, 3319–3330
Stereocontrol in a Combined Allylic Azide Rearrangement and Intramolecular Schmidt Reaction
Ruzhang Liu, Osvaldo Gutierrez, Dean J. Tantillo, and Jeffrey Aubé
Journal of the American Chemical Society, 2012, 134, 6528–6531
A Competitive Nucleotide Binding Inhibitor: In vitro Characterization of Rab7 GTPase Inhibition
A Competitive Nucleotide Binding Inhibitor: In vitro Characterization of Rab7 GTPase Inhibition
ACS Chemical Biology, 2012, 7, 1095–1108
Parallel Solid Phase Synthesis of Diaryltriazoles
Matthias Wrobel, Jeffrey Aubé, and Burkhard König
Beilstein Journal of Organic Chemistry, 2012, 8, 1027–1036
Minor Withanolides of Physalis longifolia: Structure and Cytotoxicity
Minor Withanolides of Physalis longifolia: Structure and Cytotoxicity
Chemical and Pharmaceutical Bulletin, 2012, 60, 1234–1239
Copper-Catalyzed Oxaziridine-Mediated Oxidation of C–H Bonds
Hashim F. Motiwala, Belgin Gülgeze, and Jeffrey Aubé
Journal of Organic Chemistry, 2012, 77, 7005–7022
Automated Three-Component Synthesis of a Library of  Lactams
Erik Fenster, David Hill, Oliver Reiser, and Jeffrey Aubé
Beilstein Journal of Organic Chemistry, 2012, 8, 1804–1813
(S)-N-(2,5-Dimethylphenyl)-1-(quinoline-8-ylsulfonyl)pyrrolidine-2-carboxamide as a Small Molecule Inhibitor Probe for the Study of Respiratory Syncytial Virus Infection
Blake P. Moore, Dong Hoon Chung, Daljit S. Matharu, Jennifer E. Golden, Clinton Maddox, Lynn Rasmussen, James W. Noah, Melinda I. Sosa, Subramaniam Ananthan, Nichole, A. Tower, E. Lucile White, Fuli Jia, Thomas E. Prisinzano, Jeffrey Aubé, Colleen B. Jonsson, and William E. Severson
Journal of Medicinal Chemistry, 2012, 55, 8582–8587
A Selective ATP-Binding Cassette Subfamily G Member 2 Efflux Inhibitor Revealed via High-Throughput Flow Cytometry
J. Jacob Strouse, Irena Ivnitski-Steele, Hadya M. Khawaja, Dominique Perez, Jerec Ricci, Tuanli Yao, Warren S. Weiner, Chad E. Schroeder, Denise S. Simpson, Brooks E. Maki, Kelin Li, Jennifer E. Golden, Terry D. Foutz, Anna Waller, Annette M. Evangelisti, Susan M.Young, Stephanie E. Chavez, Matthew J. Garcia, Oleg Ursu, Cristian G. Bologa, Mark B. Carter, Virginia M. Salas, Kristine Gouveia George P.Tegos, Tudor I. Oprea, Bruce S. Edwards, Jeffrey Aubé, Richard S. Larson, and Larry A. Sklar
, Journal of Biomolecular Screening, 2013, 18, 26–38
Characterization of a Cdc42 GTPase Inhibitor and its Use as a Molecular Probe
Hong, S. Ray Kenney, Genevieve K. Philips, Denise Simpson, Chad E. Schroeder, Julica Noth, Elsa Romero, Scarlett Swanson, Anna Waller, J. Jacob Strouse, Mark Carter, Alexandre Chigaev, Oleg Ursu, Tudor Oprea, Brian Hjelle, Jennifer E. Golden, Jeffrey Aubé, Laurie G. Hudson, Tione Buranda, Larry A. Sklar, and Angela Wandinger-Ness
Journal of Biological Chemistry, 2013, 288, 8531–8543

Small-molecule Pyrimidine Inhibitors of the Cdc2-like (Clk) and Dual Specificity Tyrosine Phosphorylation-regulated (Dyrk) Kinases: Development of Chemical Probe ML315
Thomas C. Coombs, Cordelle Tanega, Min Shen, Jenna L. Wang, Douglas S. Auld, Samuel W. Gerritz, Frank J. Schoenen, Craig J. Thomas, and Jeffrey Aubé
Bioorganic and Medicinal Chemistry Letters, 2013, 23, 3654–3661
The Chemistry of Bridged Lactams and Related Heterocycles
Michal Szostak and Jeffrey Aubé
Chemical Reviews, 2013, 113, 5701–5765
Benzylmorpholine Analogs as Selective Inhibitors of Lung Cytochrome P450 2A13 for the Chemoprevention of Lung Cancer in Tobacco Users
Benzylmorpholine Analogs as Selective Inhibitors of Lung Cytochrome P450 2A13 for the Chemoprevention of Lung Cancer in Tobacco Users
Pharmaceutical Research, 2013, 30, 2290-2302
Overcoming Product Inhibition in Catalysis of the Intramolecular Schmidt Reaction
Hashim Motiwala, Charlie Fehl, Sze-Wan Li, Erin Hirt, Patrick Porubsky, and Jeffrey Aubé
Journal of the American Chemical Society, 2013, 135, 9000–9009

Synthesis and Cytotoxicity of Semisynthetic Withalongolide A Analogues
Hashim F. Motiwala, Joseph Bazzill, Abbas Samadi, Huaping Zhang, Barbara N. Timmermann, Mark S. Cohen, and Jeffrey Aubé
ACS Medicinal Chemistry Letters, 2013, 4, 1069-1073
Chemotype-selective Modes of Action of -Opioid Receptor Agonists
Eyal Vardy, Philip D. Mosier, Kevin J. Frankowski, Huixian Wu, Vsevolod Katritch, Richard B. Westkaemper, Jeffrey Aubé, Raymond C. Stevens, and Bryan L. Roth
Journal of Biological Chemistry, 2013, 288, 34470-34483
Development of Functionally Selective, Small Molecule Agonists at Kappa Opioid Receptors
Lei Zhou, Kimberly M. Lovell, Kevin J. Frankowski, Stephen R. Slauson, Angela M. Phillips, John M. Streicher, Edward Stahl, Cullen L. Schmid, Peter Hodder, Franck Madoux, Michael D. Cameron, Thomas E. Prisinzano, Jeffrey Aubé, Laura M. Bohn
Journal of Biological Chemistry, 2013, 288, 36703-36716
Aryl Nitrenium Ions from N-Alkyl-N-arylamino-diazonium Precursors: Synthesis and Reactivity
Chan Woo Huh and Jeffrey Aubé
Chemical Science, 2014, 5, 699–706
Probing Chemical Space with Alkaloid-Inspired Libraries
Michael C. McLeod, Gurpreet Singh, James N. Plampin III, Digamber Rane, Jenna L. Wang, Victor W. Day, and Jeffrey Aubé
Nature Chemistry, 2014, 6, 133–140
Stereodivergent Synthesis of Enantioenriched 4-Hydroxy-2-cyclopentenones
Gurpreet Singh, Angelica Meyer, and Jeffrey Aubé
Journal of Organic Chemistry, 2014, 79, 452–458
A Concomitant Allylic Azide Rearrangement/Intramolecular Azide–Alkyne Cycloaddition Sequence
Rakesh H. Vekariya, Ruzhang Liu, and Jeffrey Aubé
Organic Letters, 2014, 16, 1844-1847
Potent and Selective Inhibitors of the TASK-1 Potassium Channel Through Chemical Optimization of a Bis-Amide Scaffold
Daniel P. Flaherty, Denise S. Simpson, Melissa Miller, Brooks E. Maki, Beiyan Zou, Jie Shi, Meng Wu, Owen B. Mcmanus, Jeffrey Aubé, Min Li, and Jennifer E. Golden
Bioorganic and Medicinal Chemistry Letters, 2014, 24, 3968–3973
Enabling Technologies in High Throughput Chemistry
Jeffrey Aubé, Steven A. Rogers, and Conrad Santini
Oxford: Elsevier, 2014, pp. 1–27

3-Substituted Biquinolinium Inhibitors of AraC Family Transcriptional Activator VirF from S. flexneri Obtained Through In Situ Chemical Ionization of 3,4-Disubstituted Dihydroquinolines
Prashi Jain, Jiaqin Li, Patrick Porubsky, Benjamin Neuenswander, Susan M. Egan, Jeffrey Aubé, and Steven Rogers
RSC Advances, 2014, 4, 39809-39816
Development of (E)-2-((1,4-dimethylpiperazin-2-ylidene)amino)-5-nitro-N-phenylbenzamide, ML336: Novel 2-Amidinophenylbenzamides as Potent Inhibitors of Venezuelan Equine Encephalitis Virus
Chad Schroeder, Tuanli Yao, Julie Sotsky, Robert Smith, Sudeshna Roy, Yong-Kyu Chu, Haixun Guo, Nichole Tower, James Noah, Sarah McKellip, Melinda Sosa, Lynn Rasmussen, Layton Smith, E. Lucile White, Jeffrey Aubé, Colleen Jonsson, Donghoon Chung, and Jennifer Golden
Journal of Medicinal Chemistry, 2014, 57, 8608–8621
Hofmann, Curtius, Schmidt, Lossen and Related reactions
Jeffrey Aubé, Charlie Fehl, Ruzhang Liu, Michael McLeod, and Hashim Motiwala
Oxford: Elsevier, 2014, pp. 598–635

Publications