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