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1

Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation

Qi Sun, Dr. Jason P. Burke, Prof. Jason Phan, Michael C. Burns, Prof. Edward T. Olejniczak, Prof. Alex G. Waterson, Prof. Taekyu Lee, Prof. Olivia W. Rossanese, Prof. Stephen W. Fesik

Journal:

Angewandte Chemie

Year:

2012

Language:

english

File:

PDF, 1.36 MB

english, 2012

2

Room-Temperature Pd-Catalyzed Amidation of Aryl Bromides Using tert- Butyl Carbamate

Bhagwanth, Swapna, Waterson, Alex G., Adjabeng, George M., Hornberger, Keith R.

Journal:

Journal of Organic Chemistry

Year:

2009

Language:

english

File:

PDF, 122 KB

english, 2009

3

ML327 Blocks N-MYC Expression and Tumor Formation in MYCN-Amplified Neuroblastomas

Rellinger, Eric J., Padmanabhan, Chandrasekhar, Craig, Brian T., An, Hanbing, Qiao, Jingbo, Waterson, Alex G., Lindsley, Craig W., Beauchamp, R. Daniel, Chung, Dai H.

Journal:

Journal of the American College of Surgeons

Year:

2016

Language:

english

File:

PDF, 144 KB

english, 2016

4

High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling

Burns, Michael C., Howes, Jennifer E., Sun, Qi, Little, Andrew J., Camper, DeMarco V., Abbott, Jason R., Phan, Jason, Lee, Taekyu, Waterson, Alex G., Rossanese, Olivia W., Fesik, Stephen W.

Journal:

Analytical Biochemistry

Year:

2018

Language:

english

File:

PDF, 1.33 MB

english, 2018

5

Discovery of Quinazolines That Activate SOS1-Mediated Nucleotide Exchange on RAS

Abbott, Jason R., Patel, Pratiq A., Howes, Jennifer E., Akan, Denis T., Kennedy, J. Phillip, Burns, Michael C., Browning, Carrie F., Sun, Qi, Rossanese, Olivia W., Phan, Jason, Waterson, Alex G., Fesi

Journal:

ACS Medicinal Chemistry Letters

Year:

2018

Language:

english

File:

PDF, 1.01 MB

english, 2018

6

ChemInform Abstract: Studies Dealing with Thionium Ion Promoted Mannich Cyclization Reactions.

Albert Padwa, Alex G. Waterson

Journal:

Year:

2000

File:

PDF, 32 KB

2000

7

ChemInform Abstract: Synthesis of Nitrogen Heterocycles Using the Intramolecular Pummerer Reaction

Albert Padwa, Alex G. Waterson

Journal:

Year:

2000

File:

PDF, 24 KB

2000

8

ChemInform Abstract: The Thionium/N-Acyliminium Ion Cyclization Cascade as a Strategy for the Synthesis of Azapolycyclic Ring Systems.

Albert Padwa, Alex G. Waterson

Journal:

Year:

2001

File:

PDF, 39 KB

2001

9

ChemInform Abstract: Studies Directed Toward the Synthesis of Viridenomycin. Route 2: A Second Generation Approach.

Alex G. Waterson, Albert W. Kruger, A. I. Meyers

Journal:

Year:

2001

File:

PDF, 34 KB

2001

10

ChemInform Abstract: Conjugate Addition of Sodium Methanesulfinate to Vinyl Pyridines and Diazines for the Synthesis of Aliphatic Sulfones.

Gregory M. Schaaf, Sabuj Mukherjee, Alex G. Waterson

Journal:

Year:

2009

File:

PDF, 51 KB

2009

11

ChemInform Abstract: Room-Temperature Pd-Catalyzed Amidation of Aryl Bromides Using tert-Butyl Carbamate.

Swapna Bhagwanth, Alex G. Waterson, George M. Adjabeng, Keith R. Hornberger

Journal:

Year:

2009

File:

PDF, 23 KB

2009

12

Dual EGFR/ErbB-2 inhibitors from novel pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines

Robert D. Hubbard, Scott H. Dickerson, Holly K. Emerson, Robert J. Griffin, Michael J. Reno, Keith R. Hornberger, David W. Rusnak, Edgar R. Wood, David E. Uehling, Alex G. Waterson

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2008

Language:

english

File:

PDF, 184 KB

english, 2008

13

Synthesis and evaluation of aniline headgroups for alkynyl thienopyrimidine dual EGFR/ErbB-2 kinase inhibitors

Alex G. Waterson, Kimberly G. Petrov, Keith R. Hornberger, Robert D. Hubbard, Douglas M. Sammond, Stephon C. Smith, Hamilton D. Dickson, Thomas R. Caferro, Kevin W. Hinkle, Kirk L. Stevens, Scott H. D

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2009

Language:

english

File:

PDF, 1.32 MB

english, 2009

14

Conjugate addition of sodium methanesulfinate to vinyl pyridines and diazines for the synthesis of aliphatic sulfones

Gregory M. Schaaf, Sabuj Mukherjee, Alex G. Waterson

Journal:

Tetrahedron Letters

Year:

2009

Language:

english

File:

PDF, 2.28 MB

english, 2009

15

The Thionium/N-Acyliminium Ion Cyclization Cascade as a Strategy for the Synthesis of Azapolycyclic Ring Systems

Albert Padwa, Alex G. Waterson

Journal:

Year:

2000

Language:

english

File:

PDF, 235 KB

english, 2000

16

Studies directed toward the synthesis of viridenomycin. Route 2: a second generation approach

Alex G Waterson, Albert W Kruger, A.I Meyers

Journal:

Tetrahedron Letters

Year:

2001

Language:

english

File:

PDF, 67 KB

english, 2001

17

Alkynyl pyrimidines as dual EGFR/ErbB2 kinase inhibitors

Alex G. Waterson, Kirk L. Stevens, Michael J. Reno, Yue-Mei Zhang, Eric E. Boros, Frederic Bouvier, Abdullah Rastagar, David E. Uehling, Scott H. Dickerson, Bryan Reep, Octerloney B. McDonald, Edgar R

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2006

Language:

english

File:

PDF, 236 KB

english, 2006

18

Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α

Thorne, Curtis A, Hanson, Alison J, Schneider, Judsen, Tahinci, Emilios, Orton, Darren, Cselenyi, Christopher S, Jernigan, Kristin K, Meyers, Kelly C, Hang, Brian I, Waterson, Alex G

Journal:

Nature Chemical Biology

Year:

2010

Language:

english

File:

PDF, 895 KB

english, 2010

19

Synthesis of the perhydroindole nucleus by a Pummerer/Mannich induced cyclization cascade

Albert Padwa, Alex G. Waterson

Journal:

Tetrahedron Letters

Year:

1998

Language:

english

File:

PDF, 224 KB

english, 1998

20

Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation

Qi Sun, Dr. Jason P. Burke, Prof. Jason Phan, Michael C. Burns, Prof. Edward T. Olejniczak, Prof. Alex G. Waterson, Prof. Taekyu Lee, Prof. Olivia W. Rossanese, Prof. Stephen W. Fesik

Journal:

Angewandte Chemie International Edition

Year:

2012

Language:

english

File:

PDF, 1.37 MB

english, 2012

21

Further optimization of the K-Cl cotransporter KCC2 antagonist ML077: Development of a highly selective and more potent in vitro probe

Eric Delpire, Aleksandra Baranczak, Alex G. Waterson, Kwangho Kim, Nathan Kett, Ryan D. Morrison, J. Scott Daniels, C. David Weaver, Craig W. Lindsley

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2012

Language:

english

File:

PDF, 1.22 MB

english, 2012

22

Discovery of Dabrafenib: A Selective Inhibitor of Raf Kinases with Antitumor Activity against B-Raf-Driven Tumors

Rheault, Tara R., Stellwagen, John C., Adjabeng, George M., Hornberger, Keith R., Petrov, Kimberly G., Waterson, Alex G., Dickerson, Scott H., Mook, Robert A., Laquerre, Sylvie G., King, Alastair J.,

Journal:

ACS Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 815 KB

english, 2013

23

Discovery of Protein–Protein Interaction Inhibitors of Replication Protein A

Patrone, James D., Kennedy, J. Phillip, Frank, Andreas O., Feldkamp, Michael D., Vangamudi, Bhavatarini, Pelz, Nicholas F., Rossanese, Olivia W., Waterson, Alex G., Chazin, Walter J., Fesik, Stephen W

Journal:

ACS Medicinal Chemistry Letters

Year:

2013

Language:

english

File:

PDF, 3.75 MB

english, 2013

24

Diels−Alder Reaction of 2-Amino-Substituted Furans as a Method for Preparing Substituted Anilines

Padwa, Albert, Dimitroff, Martin, Waterson, Alex G., Wu, Tianhua

Journal:

Journal of Organic Chemistry

Year:

1997

Language:

english

File:

PDF, 417 KB

english, 1997

25

Surface Reengineering of RPA70N Enables Cocrystallization with an Inhibitor of the Replication Protein A Interaction Motif of ATR Interacting Protein

Feldkamp, Michael D., Frank, Andreas O., Kennedy, J. Phillip, Patrone, James D., Vangamudi, Bhavatarini, Waterson, Alex G., Fesik, Stephen W., Chazin, Walter J.

Journal:

Year:

2013

Language:

english

File:

PDF, 1.36 MB

english, 2013

26

Studies Dealing with Thionium Ion Promoted Mannich Cyclization Reactions

Padwa, Albert, Waterson, Alex G.

Journal:

Journal of Organic Chemistry

Year:

2000

Language:

english

File:

PDF, 328 KB

english, 2000

27

Discovery of a Potent Inhibitor of Replication Protein A Protein–Protein Interactions Using a Fragment-Linking Approach

Frank, Andreas O., Feldkamp, Michael D., Kennedy, J. Phillip, Waterson, Alex G., Pelz, Nicholas F., Patrone, James D., Vangamudi, Bhavatarini, Camper, DeMarco V., Rossanese, Olivia W., Chazin, Walter

Journal:

Journal of Medicinal Chemistry

Year:

2013

Language:

english

File:

PDF, 3.33 MB

english, 2013

28

Narrow SAR in odorant sensing Orco receptor agonists

Romaine, Ian M., Taylor, Robert W., Saidu, Samsudeen P., Kim, Kwangho, Sulikowski, Gary A., Zwiebel, Laurence J., Waterson, Alex G.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2014

Language:

english

File:

PDF, 437 KB

english, 2014

29

Bicyclic Lactams as Chiral Homoenolate Equivalents: Synthesis of (−)-Penienone

Waterson, Alex G., Meyers, A. I.

Journal:

Journal of Organic Chemistry

Year:

2000

Language:

english

File:

PDF, 57 KB

english, 2000

30

Discovery of a Potent Stapled Helix Peptide That Binds to the 70N Domain of Replication Protein A

Frank, Andreas O., Vangamudi, Bhavatarini, Feldkamp, Michael D., Souza-Fagundes, Elaine M., Luzwick, Jessica W., Cortez, David, Olejniczak, Edward T., Waterson, Alex G., Rossanese, Olivia W., Chazin,

Journal:

Journal of Medicinal Chemistry

Year:

2014

Language:

english

File:

PDF, 2.94 MB

english, 2014

31

IMDAF Cycloaddition as a Method for the Preparation of Pyrrolophenanthridine Alkaloids

Padwa, Albert, Dimitroff, Martin, Waterson, Alex G., Wu, Tianhua

Journal:

Journal of Organic Chemistry

Year:

1998

Language:

english

File:

PDF, 162 KB

english, 1998

32

Structure–Activity Relationship of a Broad-Spectrum Insect Odorant Receptor Agonist

Taylor, Robert W., Romaine, Ian M., Liu, Chao, Murthi, Poornima, Jones, Patrick L., Waterson, Alex G., Sulikowski, Gary A., Zwiebel, Laurence J.

Journal:

ACS Chemical Biology

Year:

2012

Language:

english

File:

PDF, 591 KB

english, 2012

33

Identification and Optimization of Small Molecules That Restore E-Cadherin Expression and Reduce Invasion in Colorectal Carcinoma Cells

Stoops, Sydney L., Pearson, A. Scott, Weaver, Connie, Waterson, Alex G., Days, Emily, Farmer, Chris, Brady, Suzanne, Weaver, C. David, Beauchamp, R. Daniel, Lindsley, Craig W.

Journal:

ACS Chemical Biology

Year:

2011

Language:

english

File:

PDF, 4.95 MB

english, 2011

34

Studies Dealing with Thionim Ion Promoted Mannich Cyclization Reactions. %Page 238. The transformation of structures 29 / 30 to 31 / 32 in Scheme 9 was incorrectly drawn. This scheme should be modified as indicated below. We thank Professor Stephen Martin, University of Texas, for pointing this out to us. 06/20/2003

Padwa, Albert, Waterson, Alex G.

Journal:

Journal of Organic Chemistry

Year:

2003

Language:

english

File:

PDF, 19 KB

english, 2003

35

Diphenylpyrazoles as Replication Protein A Inhibitors

Waterson, Alex G., Kennedy, J. Phillip, Patrone, James D., Pelz, Nicholas F., Feldkamp, Michael D., Frank, Andreas O., Vangamudi, Bhavatarini, Souza-Fagundes, Elaine M., Rossanese, Olivia W., Chazin,

Journal:

ACS Medicinal Chemistry Letters

Year:

2015

Language:

english

File:

PDF, 1.39 MB

english, 2015

36

Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

Burns, Michael C., Sun, Qi, Daniels, R. Nathan, Camper, DeMarco, Kennedy, J. Phillip, Phan, Jason, Olejniczak, Edward T., Lee, Taekyu, Waterson, Alex G., Rossanese, Olivia W., Fesik, Stephen W.

Journal:

Proceedings of the National Academy of Sciences

Year:

2014

Language:

english

File:

PDF, 1.30 MB

english, 2014

37

Synthesis of Nitrogen Heterocycles Using the Intramolecular Pummerer Reaction

Padwa, Albert, Waterson, Alex

Journal:

Current Organic Chemistry

Year:

2000

Language:

english

File:

PDF, 183 KB

english, 2000

38

Recent Advancements in the Discovery of Protein-Protein Interaction Inhibitors of Replication Protein A

Patrone, James, Waterson, Alex, Fesik, Stephen

Journal:

Year:

2016

Language:

english

File:

PDF, 1.09 MB

english, 2016

39

Isoxazole-Based Small Molecule Induces Apoptosis and Sensitizes Ewing Sarcoma Cells to Tumor Necrosis Factor-Related Apoptosis-Inducing Ligand

Rellinger, Eric J., Padmanabhan, Chandrasekhar, Qiao, Jingbo, An, Hanbing, Waterson, Alex G., Lindsley, Craig W., Beauchamp, R. Daniel, Chung, Dai H.

Journal:

Journal of the American College of Surgeons

Year:

2017

Language:

english

File:

PDF, 161 KB

english, 2017

40

Small molecule-mediated activation of RAS elicits biphasic modulation of phospho ERK levels that are regulated through negative feedback on SOS1

Howes, Jennifer E., Akan, Denis T., Burns, Michael C., Rossanese, Olivia W., Waterson, Alex G., Fesik, Stephen W.

Journal:

Molecular Cancer Therapeutics

Year:

2018

Language:

english

File:

PDF, 2.78 MB

english, 2018

41

Allosteric Antagonism of Insect Odorant Receptor Ion Channels

Jones, Patrick L., Pask, Gregory M., Romaine, Ian M., Taylor, Robert W., Reid, Paul R., Waterson, Alex G., Sulikowski, Gary A., Zwiebel, Laurence J., Nighorn, Alan

Journal:

Year:

2012

Language:

english

File:

PDF, 881 KB

english, 2012

42

cFLIP critically modulates apoptotic resistance in epithelial-to-mesenchymal transition

Padmanabhan, Chandrasekhar, Rellinger, Eric J., Zhu, Jing, An, Hanbing, Woodbury, Luke G., Chung, Dai H., Waterson, Alex G., Lindsley, Craig W., Means, Anna L., Beauchamp, R. Daniel

Journal:

Year:

2017

Language:

english

File:

PDF, 13.33 MB

english, 2017

43

Dual inhibition of Kif15 by oxindole and quinazolinedione chemical probes

Dumas, Megan E., Chen, Geng-Yuan, Kendrick, Nicole D., Xu, George, Larsen, Scott A., Jana, Somnath, Waterson, Alex G., Bauer, Joshua A., Hancock, William, Sulikowski, Gary A., Ohi, Ryoma

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2018

Language:

english

File:

PDF, 3.48 MB

english, 2018

44

Isoform selective PLD inhibition by novel, chiral 2,8-diazaspiro[4.5]decan-1-one derivatives

Waterson, Alex G., Scott, Sarah A., Kett, Nathan R., Blobaum, Anna L., Alex Brown, H., Lindsley, Craig W.

Journal:

Bioorganic & Medicinal Chemistry Letters

Year:

2018

Language:

english

File:

PDF, 1.10 MB

english, 2018

45

Novel polymers from atom transfer polymerisation mediated by copper(I) Schiff base complexes

Haddleton, David M., Heming, Alex M., Jarvis, Adam P., Khan, Afzal, Marsh, Andrew, Perrier, Sebastien, Bon, Stefan A.F., Jackson, Stuart G., Edmonds, Ryan, Kelly, Elizabeth, Kukulj, Dax, Waterson, Car

Journal:

Macromolecular Symposia

Year:

2000

File:

PDF, 916 KB

2000

46

Small molecule SOS1 agonists modulate MAPK and PI3K signaling via independent cellular responses

Akan, Denis T., Howes, Jennifer E., Sai, Jiqing, Arnold, Allison L., Beesetty, Yugandhar, Phan, Jason, Olejniczak, Edward T, Waterson, Alex G., Fesik, Stephen W.

Journal:

ACS Chemical Biology

Year:

2019

File:

PDF, 3.52 MB

2019

47

Discovery of Sulfonamide-Derived Agonists of SOS1-Mediated Nucleotide Exchange on RAS Using Fragment-Based Methods

Sarkar, Dhruba, Olejniczak, Edward T, Phan, Jason, Coker, Jesse A, Sai, Jiqing, Arnold, Allison L, Beesetty, Yugandhar, Waterson, Alex G., Fesik, Stephen W.

Journal:

Journal of Medicinal Chemistry

Year:

2020

File:

PDF, 958 KB

2020