• 1166 Citations
  • 15 h-Index
19952019

Research output per year

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Research Output

  • 1166 Citations
  • 15 h-Index
  • 25 Article
  • 1 Conference article
2019

L-Type amino acid transporter 1 activity of 1,2,3-triazolyl analogs of L-histidine and L-tryptophan

Hall, C., Wolfe, H., Wells, A., Chien, H. C., Colas, C., Schlessinger, A., Giacomini, K. M. & Thomas, A. A., Aug 15 2019, In : Bioorganic and Medicinal Chemistry Letters. 29, 16, p. 2254-2258 5 p.

Research output: Contribution to journalArticle

4 Scopus citations
2018

Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1)

Chien, H. C., Colas, C., Finke, K., Springer, S., Stoner, L., Zur, A. A., Venteicher, B., Campbell, J., Hall, C., Flint, A., Augustyn, E., Hernandez, C., Heeren, N., Hansen, L., Anthony, A., Bauer, J., Fotiadis, D., Schlessinger, A., Giacomini, K. M. & Thomas, A. A., Aug 23 2018, In : Journal of Medicinal Chemistry. 61, 16, p. 7358-7373 16 p.

Research output: Contribution to journalArticle

15 Scopus citations
2016

LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates

Zur, A. A., Chien, H. C., Augustyn, E., Flint, A., Heeren, N., Finke, K., Hernandez, C., Hansen, L., Miller, S., Lin, L., Giacomini, K. M., Colas, C., Schlessinger, A. & Thomas, A. A., Jan 1 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 20, p. 5000-5006 7 p.

Research output: Contribution to journalArticle

20 Scopus citations

LAT-1 activity of meta-substituted phenylalanine and tyrosine analogs

Augustyn, E., Finke, K., Zur, A. A., Hansen, L., Heeren, N., Chien, H. C., Lin, L., Giacomini, K. M., Colas, C., Schlessinger, A. & Thomas, A. A., Jun 1 2016, In : Bioorganic and Medicinal Chemistry Letters. 26, 11, p. 2616-2621 6 p.

Research output: Contribution to journalArticle

22 Scopus citations
2015

Mitigation of opioid off-target effects and identification of structural drivers of opioid receptor engagement for BACE-1 small molecule inhibitors

Diaz, D., Dambach, D., Siu, M., Hunt, K., Thomas, A., Lyssikatos, J., Liu, X., Lewin-Koh, S., Mccray, B. & Ford, K., Jul 24 2015, In : Toxicology Mechanisms and Methods. 25, 6, p. 478-486 9 p.

Research output: Contribution to journalArticle

2 Scopus citations
2014

8-tetrahydropyran-2-yl chromans: Highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors

Thomas, A. A., Hunt, K. W., Newhouse, B., Watts, R. J., Liu, X., Vigers, G., Smith, D., Rhodes, S. P., Brown, K. D., Otten, J. N., Burkard, M., Cox, A. A., Geck Do, M. K., Dutcher, D., Rana, S., Delisle, R. K., Regal, K., Wright, A. D., Groneberg, R., Liao, J. & 4 others, Scearce-Levie, K., Siu, M., Purkey, H. E. & Lyssikatos, J. P., Dec 11 2014, In : Journal of Medicinal Chemistry. 57, 23, p. 10112-10129 18 p.

Research output: Contribution to journalArticle

11 Scopus citations

Discovery of 5,6,7,8-tetrahydropyrido[3,4-d]pyrimidine inhibitors of Erk2

Blake, J. F., Gaudino, J. J., De Meese, J., Mohr, P., Chicarelli, M., Tian, H., Garrey, R., Thomas, A., Siedem, C. S., Welch, M. B., Kolakowski, G., Kaus, R., Burkard, M., Martinson, M., Chen, H., Dean, B., Dudley, D. A., Gould, S. E., Pacheco, P., Shahidi-Latham, S. & 5 others, Wang, W., West, K., Yin, J., Moffat, J. & Schwarz, J. B., Jun 15 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 12, p. 2635-2639 5 p.

Research output: Contribution to journalArticle

21 Scopus citations

Discovery of 7-tetrahydropyran-2-yl chromans: β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors that reduce amyloid β-protein (Aβ) in the central nervous system

Thomas, A. A., Hunt, K. W., Volgraf, M., Watts, R. J., Liu, X., Vigers, G., Smith, D., Sammond, D., Tang, T. P., Rhodes, S. P., Metcalf, A. T., Brown, K. D., Otten, J. N., Burkard, M., Cox, A. A., Do, M. K. G., Dutcher, D., Rana, S., Delisle, R. K., Regal, K. & 7 others, Wright, A. D., Groneberg, R., Scearce-Levie, K., Siu, M., Purkey, H. E., Lyssikatos, J. P. & Gunawardana, I. W., Jan 7 2014, In : Journal of Medicinal Chemistry. 57, 3, p. 878-902 25 p.

Research output: Contribution to journalArticle

31 Scopus citations

Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors

Volgraf, M., Chan, L., Huestis, M. P., Purkey, H. E., Burkard, M., Geck Do, M., Harris, J., Hunt, K. W., Liu, X., Lyssikatos, J. P., Rana, S., Thomas, A. A., Vigers, G. P. A. & Siu, M., Jun 1 2014, In : Bioorganic and Medicinal Chemistry Letters. 24, 11, p. 2477-2480 4 p.

Research output: Contribution to journalArticle

11 Scopus citations
2013

Mechanistic Pharmacokinetic-Pharmacodynamic Modeling of BACE1 Inhibition in Monkeys: Development of a Predictive Model for Amyloid Precursor Protein Processings

Liu, X., Wong, H., Scearce-Levie, K., Watts, R. J., Coraggio, M., Shin, Y. G., Peng, K., Wildsmith, K. R., Atwal, J. K., Mango, J., Schauer, S. P., Regal, K., Hunt, K. W., Thomas, A. A., Siu, M., Lyssikatos, J., Deshmukh, G. & Hop, C. E. C. A., Jul 1 2013, In : Drug Metabolism and Disposition. 41, 7, p. 1319-1328 10 p.

Research output: Contribution to journalArticle

13 Scopus citations

Spirocyclic β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: From hit to lowering of cerebrospinal fluid (CSF) amyloid β in a higher species

Hunt, K. W., Cook, A. W., Watts, R. J., Clark, C. T., Vigers, G., Smith, D., Metcalf, A. T., Gunawardana, I. W., Burkard, M., Cox, A. A., Geck Do, M. K., Dutcher, D., Thomas, A. A., Rana, S., Kallan, N. C., Delisle, R. K., Rizzi, J. P., Regal, K., Sammond, D., Groneberg, R. & 6 others, Siu, M., Purkey, H., Lyssikatos, J. P., Marlow, A., Liu, X. & Tang, T. P., Apr 25 2013, In : Journal of Medicinal Chemistry. 56, 8, p. 3379-3403 25 p.

Research output: Contribution to journalArticle

47 Scopus citations
2008

Non-charged thiamine analogs as inhibitors of enzyme transketolase

Thomas, A. A., De Meese, J., Le Huerou, Y., Boyd, S. A., Romoff, T. T., Gonzales, S. S., Gunawardana, I., Kaplan, T., Sullivan, F., Condroski, K., Lyssikatos, J. P., Aicher, T. D., Ballard, J., Bernat, B., DeWolf, W., Han, M., Lemieux, C., Smith, D., Weiler, S., Wright, S. K. & 2 others, Vigers, G. & Brandhuber, B., Jan 15 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 2, p. 509-512 4 p.

Research output: Contribution to journalArticle

26 Scopus citations

Prodrug thiamine analogs as inhibitors of the enzyme transketolase

Le Huerou, Y., Gunawardana, I., Thomas, A. A., Boyd, S. A., de Meese, J., deWolf, W., Gonzales, S. S., Han, M., Hayter, L., Kaplan, T., Lemieux, C., Lee, P., Pheneger, J., Poch, G., Romoff, T. T., Sullivan, F., Weiler, S., Wright, S. K. & Lin, J., Jan 15 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 2, p. 505-508 4 p.

Research output: Contribution to journalArticle

17 Scopus citations

Synthesis, in vitro and in vivo activity of thiamine antagonist transketolase inhibitors

Thomas, A. A., Le Huerou, Y., De Meese, J., Gunawardana, I., Kaplan, T., Romoff, T. T., Gonzales, S. S., Condroski, K., Boyd, S. A., Ballard, J., Bernat, B., DeWolf, W., Han, M., Lee, P., Lemieux, C., Pedersen, R., Pheneger, J., Poch, G., Smith, D., Sullivan, F. & 5 others, Weiler, S., Wright, S. K., Lin, J., Brandhuber, B. & Vigers, G., Mar 15 2008, In : Bioorganic and Medicinal Chemistry Letters. 18, 6, p. 2206-2210 5 p.

Research output: Contribution to journalArticle

36 Scopus citations
2005

Oligo-α-hydroxy ester cross-linkers: Impact of cross-linker structure on biodegradable hydrogel networks

Eichenbaum, K. D., Thomas, A. A., Eichenbaum, G. M., Gibney, B. R., Needham, D. & Kiser, P. F., Dec 27 2005, In : Macromolecules. 38, 26, p. 10757-10762 6 p.

Research output: Contribution to journalArticle

22 Scopus citations

Symmetrical biodegradable crosslinkers for use in polymeric devices

Thomas, A. A., Kim, I. T. & Kiser, P. F., Dec 19 2005, In : Tetrahedron Letters. 46, 51, p. 8921-8925 5 p.

Research output: Contribution to journalArticle

8 Scopus citations
2002

Osmium-Catalyzed Dihydroxylation of Olefins in Acidic Media: Old Process, New Tricks

Dupau, P., Epple, R., Thomas, A. A., Fokin, V. V. & Sharpless, K. B., May 1 2002, In : Advanced Synthesis and Catalysis. 344, 3-4, p. 421-433 13 p.

Research output: Contribution to journalArticle

171 Scopus citations
2001

Isotope effects and the distinction between synchronous, asynchronous, and stepwise Diels-Alder reactions

Singleton, D. A., Schulmeier, B. E., Hang, C., Thomas, A. A., Leung, S. W. & Merrigan, S. R., Jun 11 2001, In : Tetrahedron. 57, 24, p. 5149-5160 12 p.

Research output: Contribution to journalArticle

72 Scopus citations

Rearrangement of methylenecamphor during electrophilic bromination: Remarkably clean access to the unnatural fenchyl (1,3,3-trimethylbicyclo[2.2.1]heptane) system

Thomas, A. A., Monk, K. A., Abraham, S., Lee, S. & Garner, C. M., Mar 18 2001, In : Tetrahedron Letters. 42, 12, p. 2261-2263 3 p.

Research output: Contribution to journalArticle

11 Scopus citations
2000

Design and performance of poly(HPMA) hydrogels containing symmetrical biodegradable crosslinkers composed of oligo-lactate and oligo-glycolate esters

Kiser, P. F., Thomas, A. A., Eichenbaum, G. M., Needham, D. & Kim, I., Mar 1 2000, In : American Chemical Society, Polymer Preprints, Division of Polymer Chemistry. 41, 1, p. 712-713 2 p.

Research output: Contribution to journalConference article

1 Scopus citations
1999
9 Scopus citations

The catalytic asymmetric aminohydroxylation of unsaturated phosphonates

Thomas, A. A. & Sharpless, K. B., Oct 29 1999, In : Journal of Organic Chemistry. 64, 22, p. 8379-8385 7 p.

Research output: Contribution to journalArticle

115 Scopus citations
1998

Anti-tumor activity of a platinated polymer (AP5070) - Chemical optimization and confirmation of enhanaced therapeutic ratio

Luthy, C. L., Thomas, A. A., Callahan, E. H., Van Inwegen, R. G., Wilson, G., Evagorou, E. G., Gianasi, E. & Duncan, R., Jan 1 1998, In : Proceedings of the Controlled Release Society. 25, p. 132-133 2 p.

Research output: Contribution to journalArticle

1 Scopus citations
1997

Experimental and theoretical kinetic isotope effects for asymmetric dihydroxylation. Evidence supporting a rate-limiting '(3+2)' cycloaddition

DelMonte, A. J., Haller, J., Houk, K. N., Sharpless, K. B., Singleton, D. A., Strassner, T. & Thomas, A. A., Nov 11 1997, In : Journal of the American Chemical Society. 119, 41, p. 9907-9908 2 p.

Research output: Contribution to journalArticle

210 Scopus citations
1995

Allylic Metalation of Endo- and ExoCyclic Alkenes: Anomalous High Reactivity of β-Pinene

Garner, C. M. & Thomas, A. A., Oct 1 1995, In : Journal of Organic Chemistry. 60, 21, p. 7051-7054 4 p.

Research output: Contribution to journalArticle

3 Scopus citations

High-Precision Simultaneous Determination of Multiple Small Kinetic Isotope Effects at Natural Abundance

Singleton, D. A. & Thomas, A. A., Jan 1 1995, In : Journal of the American Chemical Society. 117, 36, p. 9357-9358 2 p.

Research output: Contribution to journalArticle

267 Scopus citations