Research & Publications Updates

The Wipf Group research program focuses on:
• total synthesis of natural products
• organometallic and heterocyclic methodology development
• medicinal chemistry
• computational prediction of macroscopic properties as well as molecular modeling

For recent examples of research projects of specific group members, please browse the publication records shown below. For a pdf reference file of all Wipf Group papers from 1990-2016, please click here.

2016 Co-Worker Publication 1 Publication 2 Publication 3 Conference Presentations & Patents
  Raffaele Colombo

"Optimization of Pyrazole-Containing 1,2,4-Triazolo-[3,4-B]Thiadiazines, a New Class of STAT3 Pathway Inhibitors." Laporte, M. G.; Wang, Z.; Colombo, R.; Garzan, A.; Peshkov, V. A.; Liang, M.; Johnston, P. A.; Schurdak, M. E.; Sen, M.; Camarco, D. P.; Hua, Y.; Pollock, N. I.; Lazo, J. S.; Grandis, J. R.; Wipf, P.; Huryn, D. M. Bioorg. Med. Chem. Lett. 2016, 26, 3581-3585.

"Total Synthesis and Biological Evaluation of Tubulysin Analogues." Colombo, R.; Wang, Z.; Han, J.; Balachandran, R.; Daghestani, H. N.; Camarco, D. P.; Vogt, A.; Day, B. W.; Mendel, D.; Wipf, P. J. Org. Chem. (Special Issue on Heterocycles)2016, 81(21), 10302-10320.

  4
  Joe Salamoun

"Allosteric Modulation of Phosphatase Activity May Redefine Therapeutic Value." Salamoun, J. M.; Wipf, P. J. Med. Chem. 2016, 59(17), 7771-7772.

"Photooxygenation of an Amino-Thienopyridone Yields a More Potent PTP4A3 Inhibitor." Salamoun, J. M.; McQueeney, K. E.; Patil, K.; Geib, S. J.; Sharlow, E. R.; Lazo, J. S.; Wipf, P. Org. Biomol. Chem. 2016, 14, 6398-6402.

 

2
  Matt LaPorte

"Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway." Alverez, C.; Bulfer, S. L.; Chakrasali, R.; Chimenti, M. S.; Deshaies, R. J.; Green, N.; Kelly, M.; Laporte, M. G.; Lewis, T. S.; Liang, M.; Moore, W. J.; Neitz, R. J.; Peshkov, V. A.; Walters, M. A.; Zhang, F.; Arkin, M. R.; Wipf, P.; Huryn, D. M. ACS Med. Chem. Lett. 2016, 7, 182-187.

"Optimization of Pyrazole-Containing 1,2,4-Triazolo-[3,4-B]Thiadiazines, a New Class of STAT3 Pathway Inhibitors." Laporte, M. G.; Wang, Z.; Colombo, R.; Garzan, A.; Peshkov, V. A.; Liang, M.; Johnston, P. A.; Schurdak, M. E.; Sen, M.; Camarco, D. P.; Hua, Y.; Pollock, N. I.; Lazo, J. S.; Grandis, J. R.; Wipf, P.; Huryn, D. M. Bioorg. Med. Chem. Lett. 2016, 26, 3581-3585.   2
  Mary Liang

"Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway." Alverez, C.; Bulfer, S. L.; Chakrasali, R.; Chimenti, M. S.; Deshaies, R. J.; Green, N.; Kelly, M.; Laporte, M. G.; Lewis, T. S.; Liang, M.; Moore, W. J.; Neitz, R. J.; Peshkov, V. A.; Walters, M. A.; Zhang, F.; Arkin, M. R.; Wipf, P.; Huryn, D. M. ACS Med. Chem. Lett. 2016, 7, 182-187.

"Optimization of Pyrazole-Containing 1,2,4-Triazolo-[3,4-B]Thiadiazines, a New Class of STAT3 Pathway Inhibitors." Laporte, M. G.; Wang, Z.; Colombo, R.; Garzan, A.; Peshkov, V. A.; Liang, M.; Johnston, P. A.; Schurdak, M. E.; Sen, M.; Camarco, D. P.; Hua, Y.; Pollock, N. I.; Lazo, J. S.; Grandis, J. R.; Wipf, P.; Huryn, D. M. Bioorg. Med. Chem. Lett. 2016, 26, 3581-3585.

  2
  John Milligan

"Hydrophosphination of Bicyclo[1.1.0]butane-1-carbonitriles". Milligan, J. A.; Busacca, C. A.; Senanayake, C. H.; Wipf, P. Org. Lett. 2016, 18(17), 4300-4303.

"Click Chemistry: Straining to React." Milligan, J. A.; Wipf, P. Nat. Chem. 2016, 8, 296-297.   1
  Vsevolod Peshkov

"Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway." Alverez, C.; Bulfer, S. L.; Chakrasali, R.; Chimenti, M. S.; Deshaies, R. J.; Green, N.; Kelly, M.; Laporte, M. G.; Lewis, T. S.; Liang, M.; Moore, W. J.; Neitz, R. J.; Peshkov, V. A.; Walters, M. A.; Zhang, F.; Arkin, M. R.; Wipf, P.; Huryn, D. M. ACS Med. Chem. Lett. 2016, 7, 182-187.

"Optimization of Pyrazole-Containing 1,2,4-Triazolo-[3,4-B]Thiadiazines, a New Class of STAT3 Pathway Inhibitors." Laporte, M. G.; Wang, Z.; Colombo, R.; Garzan, A.; Peshkov, V. A.; Liang, M.; Johnston, P. A.; Schurdak, M. E.; Sen, M.; Camarco, D. P.; Hua, Y.; Pollock, N. I.; Lazo, J. S.; Grandis, J. R.; Wipf, P.; Huryn, D. M. Bioorg. Med. Chem. Lett. 2016, 26, 3581-3585.    
  Chaemin Lim

"A Mitochondrial-Targeted Nitroxide Is a Potent Inhibitor of Ferroptosis." Krainz, T.; Gaschler, M. M.; Lim, C.; Sacher, J. R.; Stockwell, B. R.; Wipf, P. ACS Cent. Sci. 2016, 2(9), 653-659.

 

 

6
  Celeste Alverez

"Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway." Alverez, C.; Bulfer, S. L.; Chakrasali, R.; Chimenti, M. S.; Deshaies, R. J.; Green, N.; Kelly, M.; Laporte, M. G.; Lewis, T. S.; Liang, M.; Moore, W. J.; Neitz, R. J.; Peshkov, V. A.; Walters, M. A.; Zhang, F.; Arkin, M. R.; Wipf, P.; Huryn, D. M. ACS Med. Chem. Lett. 2016, 7, 182-187.

 

 

3
  Erin Skoda

"Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer." Johnson, J. K.; Skoda, E. M.; Zhou, J.; Parrinello, E.; Wang, D.; O'Malley, K.; Eyer, B. R.; Kazancioglu, M. Z.; Eisermann, K.; Johnston, P. A.; Nelson, J. B.; Wang, Z.; Wipf, P. ACS Med. Chem. Lett. 2016, 7(8), 785-790.

 

  2
  James Johnson

"Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer." Johnson, J. K.; Skoda, E. M.; Zhou, J.; Parrinello, E.; Wang, D.; O'Malley, K.; Eyer, B. R.; Kazancioglu, M. Z.; Eisermann, K.; Johnston, P. A.; Nelson, J. B.; Wang, Z.; Wipf, P. ACS Med. Chem. Lett. 2016, 7(8), 785-790.

    1
  Taber Lewis

"Allosteric Indole Amide Inhibitors of p97: Identification of a Novel Probe of the Ubiquitin Pathway." Alverez, C.; Bulfer, S. L.; Chakrasali, R.; Chimenti, M. S.; Deshaies, R. J.; Green, N.; Kelly, M.; Laporte, M. G.; Lewis, T. S.; Liang, M.; Moore, W. J.; Neitz, R. J.; Peshkov, V. A.; Walters, M. A.; Zhang, F.; Arkin, M. R.; Wipf, P.; Huryn, D. M. ACS Med. Chem. Lett. 2016, 7, 182-187.

    1
  Yongzhao Yan

"2.3 Å Resolution Cryo-EM Structure of Human p97 and Mechanism of Allosteric Inhibition." Banerjee, S.; Bartesaghi, A.; Merk, A.; Rao, P.; Bulfer, S. L.; Yan, Y.; Green, N.; Mroczkowski, B.; Neitz, R. J.; Wipf, P.; Falconieri, V.; Deshaies, R. J.; Milne, J. L. S.; Huryn, D.; Arkin, M.; Subramaniam, S. Science 2016, 351(6275), 871-875.

    1
  Alex Manos-Turvey "Dihydropyrimidinones and -Thiones With Improved Activity Against Human Polyomavirus Family Members." Manos-Turvey, A.; Al-Ashtal, H. A.; Needham, P. G.; Hartline, C. B.; Prichard, M. N.; Wipf, P.; Brodsky, J. L. Bioorg. Med. Chem. Lett. 2016, 26, 5087-5091.      
  Ben Eyer "Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer." Johnson, J. K.; Skoda, E. M.; Zhou, J.; Parrinello, E.; Wang, D.; O'Malley, K.; Eyer, B. R.; Kazancioglu, M. Z.; Eisermann, K.; Johnston, P. A.; Nelson, J. B.; Wang, Z.; Wipf, P. ACS Med. Chem. Lett. 2016, 7(8), 785-790.      
  Atefeh Garzan "Optimization of Pyrazole-Containing 1,2,4-Triazolo-[3,4-B]Thiadiazines, a New Class of STAT3 Pathway Inhibitors." Laporte, M. G.; Wang, Z.; Colombo, R.; Garzan, A.; Peshkov, V. A.; Liang, M.; Johnston, P. A.; Schurdak, M. E.; Sen, M.; Camarco, D. P.; Hua, Y.; Pollock, N. I.; Lazo, J. S.; Grandis, J. R.; Wipf, P.; Huryn, D. M. Bioorg. Med. Chem. Lett. 2016, 26, 3581-3585.      
  Josh Sacher

"A Mitochondrial-Targeted Nitroxide Is a Potent Inhibitor of Ferroptosis." Krainz, T.; Gaschler, M. M.; Lim, C.; Sacher, J. R.; Stockwell, B. R.; Wipf, P. ACS Cent. Sci. 2016, 2(9), 653-659.

     
  Junyan Han "Total Synthesis and Biological Evaluation of Tubulysin Analogues." Colombo, R.; Wang, Z.; Han, J.; Balachandran, R.; Daghestani, H. N.; Camarco, D. P.; Vogt, A.; Day, B. W.; Mendel, D.; Wipf, P. J. Org. Chem. (Special Issue on Heterocycles)2016, 81(21), 10302-10320.      
  Zhiyong Wang

"Total Synthesis and Biological Evaluation of Tubulysin Analogues." Colombo, R.; Wang, Z.; Han, J.; Balachandran, R.; Daghestani, H. N.; Camarco, D. P.; Vogt, A.; Day, B. W.; Mendel, D.; Wipf, P. J. Org. Chem. (Special Issue on Heterocycles)2016, 81(21), 10302-10320..

     
  Mustafa Kazancioglu

"Small Molecule Antagonists of the Nuclear Androgen Receptor for the Treatment of Castration-Resistant Prostate Cancer." Johnson, J. K.; Skoda, E. M.; Zhou, J.; Parrinello, E.; Wang, D.; O'Malley, K.; Eyer, B. R.; Kazancioglu, M. Z.; Eisermann, K.; Johnston, P. A.; Nelson, J. B.; Wang, Z.; Wipf, P. ACS Med. Chem. Lett. 2016, 7(8), 785-790.

     
  Tanja Krainz "A Mitochondrial-Targeted Nitroxide Is a Potent Inhibitor of Ferroptosis." Krainz, T.; Gaschler, M. M.; Lim, C.; Sacher, J. R.; Stockwell, B. R.; Wipf, P. ACS Cent. Sci. 2016, 2(9), 653-659.      
  Steph McCabe "Total Synthesis, Biosynthesis and Biological Profiles of Clavine Alkaloids." McCabe, S. R.; Wipf, P. Org. Biomol. Chem. 2016, 14, 5894-5913.      
  Kalyani Patil "Photooxygenation of an Amino-Thienopyridone Yields a More Potent PTP4A3 Inhibitor." Salamoun, J. M.; McQueeney, K. E.; Patil, K.; Geib, S. J.; Sharlow, E. R.; Lazo, J. S.; Wipf, P. Org. Biomol. Chem. 2016, 14, 6398-6402.      
  Nic Reed "Synthesis and Evaluation of Potent KCNQ2/3-specific Channel Activators." Kumar, M.; Reed, N.; Liu, R.; Aizenmann, E.; Wipf, P.; Tzounopoulos, T. Mol. Pharmacol. 2016, 89(6), 667-677.      
  Ruiting Liu "Synthesis and Evaluation of Potent KCNQ2/3-specific Channel Activators." Kumar, M.; Reed, N.; Liu, R.; Aizenmann, E.; Wipf, P.; Tzounopoulos, T. Mol. Pharmacol. 2016, 89(6), 667-677.      
  Zhuzhu Wang "Optimization of Pyrazole-Containing 1,2,4-Triazolo-[3,4-B]Thiadiazines, a New Class of STAT3 Pathway Inhibitors." Laporte, M. G.; Wang, Z.; Colombo, R.; Garzan, A.; Peshkov, V. A.; Liang, M.; Johnston, P. A.; Schurdak, M. E.; Sen, M.; Camarco, D. P.; Hua, Y.; Pollock, N. I.; Lazo, J. S.; Grandis, J. R.; Wipf, P.; Huryn, D. M. Bioorg. Med. Chem. Lett. 2016, 26, 3581-3585.      
  Marina Kovaliov

 

    3
  Zhizhou Yue

 

    3
  Lalith Samankumara

 

    2
  Alex Chatterley       2
  Michael Houghton

 

    1
  Eric Miller       1