Publications

  1. Pomeroy, J., Khalifa, M., Milanes, J., Palmentiero, C., MOrris, J., & Golden, J. E. (2023). Synthesis and Evaluation of Benzylamine Inhibitors of Neuropathogenic Naegleria fowleri ‘Brain-Eating’ Amoeba. ACS Medicinal Chemistry Letters.
  2. Lish, M., Milanes, J., Sanders, K., Guzei, I., Morris, J., & Golden, J. E. (2023). Mannich‐Type Condensation and Domino Quinazolinone‐Amidine Rearrangement Affords Ring‐Fused Mackinazolinones with Anti‐Amoebic Activity. Advanced Synthesis & Catalysis365, 4567. https://doi.org/10.1002/adsc.202300994
  3. Golden, J. E. (2023). In This Issue. ACS Medicinal Chemistry Letters14(8). https://doi.org/10.1021/acsmedchemlett.3c00316
  4. Z, T., Golden, J. E., Jonsson, C., & Meibohm, B. (2023). Clinical and Translational Pharmacology Considerations for Anti-infectives Approved Under the FDA Animal Rule. . Clin Pharmacokinet. 62(7), 943-953. https://doi.org/10.1007/s40262-023-01267-x
  5. Cao, X., Yang, D., Parvathareddy , J., Chu , Y., Kim, E., Fitz-Henley , J. N., Li , X., Lukka, P. B., Parmar , K. R., Temrikar , Z. H., Dhole , P., Adcock, R. S., Gabbard, J., Bansal, S., Lee, J., Zalduondo, L., Hayes, E., Stabenow , J., Meibohm, B., … Golden, J. E. (2023). Efficacy of a brain-penetrant antiviral in lethal Venezuelan and eastern equine encephalitis mouse models. Science Translational Medicine, eabl9344. https://doi.org/10.1126/scitranslmed.abl9344
  6. Ogorek, T., & Golden, J. E. (2023). Advances in the Development of Small Molecule Antivirals Against Equine Encephalitic Alphaviruses.. Viruseshttps://doi.org/org/10.3390/v15020413
  7. Fitz-Henley, J., Rozema, S., & Golden, J. E. (2022). Dihydropyrazinoquinazolinones via SN2 Sulfamidate Ring-Opening and a Sequential Quinazolinone-Amidine Rearrangement Strategy (SQuAReS). . J Org Chem87(21), 14889-14898.
  8. Golden, J. E. (2022). In This Issue. ACS Med. Chem. Lett13(11), 1686-1687. https://doi.org/10.1021/acsmedchemlett.2c00451
  9. 4. Milanes, J., Suryadi, , J., Monaghan, , N., Harding, , E., Morris, C., Khalifa, M., Rozema, S., & Golden, J. E. (2022). Characterization of Glucokinases from Pathogenic Free-Living Amoebae. Antimicrob. Agents Chemother, e0237321.
  10. Golden, J. E., Ryan, M., Cao, X., Reichard, W., Ogorek, T., Das, P., Jonsson, C., Baudry, J., & Chung, D. (2022). Piperazinobenzodiazepinones: New Encephalitic Alphavirus Inhibitors via Ring Expansion of 2-Dichloromethylquinazolinones. ACS Med Chem Lett13(4), 546-553.
  11. Golden, J. E. (2021). Construction of N-Boc-2-Alkylaminoquinazolin-4(3H)-ones via a Three-Component, One-Pot Protocol Mediated by Copper(II) Chloride that Spares Enantiomeric Purity. Adv. Synth. Catal. https://doi.org/doi.org/10.1002/adsc.202001279
  12. Golden, J. E. (2021). Diastereoselective Multicomponent Synthesis of Ring-fused Quinazolinones via Sequential Quinazolinone Rearrangement & Intramolecular Ring Closure of (Z)-Benzamidines. Org. Lett.23(15), 5799-5803. https://doi.org/10.1021/acs.orglett.1c01955
  13. Golden, J. E. (2021). Engineering selectivity for reduced toxicity of bacterial kinase inhibitors using structure-guided medicinal chemistry. ACS Med Chem. Lett. 12(2), 228-235.
  14. Golden, J. E. (2021). Engineering Selectivity for Reduced Toxicity of Bacterial Kinase Inhibitors Using Structure-Guided Medicinal Chemistry. . ACS Med. Chem. Lett. 12, 228-235.
  15. Golden, J. E. (2021). Time to ‘Mind The Gap’ in Novel Small Molecule Drug Discovery for Direct-Acting Antivirals for SARS-CoV-2. Curr. Opin. Virol50, 1-7. https://doi.org/10.1016/j.coviro.2021.06.008
  16. Golden, J. E. (2020). Dual Stage Picolinic Acid Derived Inhibitors of Toxoplasma gondii. ACS Med. Chem. Lett. 11(12), 2382-2388.
  17. Golden, J. E. (2020). Emergence and magnitude of ML336 resistance in Venezuelan equine encephalitis virus depends on the microenvironment. J. Virologyhttps://doi.org/10.1128/JVI.00317-20.
  18. Golden, J. E. (2020). Discovery of specific inhibitors of endoplasmic reticulum aminopeptidase 1. . J Med Chem63(1), 103-121. https://doi.org/10.1021/acs.jmedchem.9b00293
  19. Golden, J. E. Divergent 2-Chloroquinazolin-4(3H)-one Rearrangement: Twisted-Cyclic Guanidines or Ring-Fused N-Acylguanidines via a Domino Process. Chemistry A European Journal26, 2486-2492. https://doi.org/10.1002/chem.201905219
  20. Golden, J. E. (2019). “In This Issue, December,” Overview and significance of three highlighted articles featured in the December 2019 issue is summarized. ACS Med. Chem. Lett, 10,12. https://doi.org/ DOI: 10.1021/acsmedchemlett.9b00545
  21. Skidmore, A. M., Adcock, R. S., Lee, J., Jonsson, C., Golden, J. E., & Chung, D. H. (2019). Benzamidine ML336 inhibits plus and minus strand RNA synthesis of Venezuelan equine encephalitis virus without affecting host RNA production. Antiviral Reshttps://doi.org/doi: 10.1016/j.antiviral.2019.104674.
  22. Khalifa, M. M., Philkhana, S., & Golden, J. E. (2019). Synthesis of Ring-Fused, N-Substituted 4-Quinolinones Using pKa-Guided, Base-Promoted Annulations with Isatoic Anhydrides: Total Synthesis of Penicinotam. J. Org. Chem85(2), 464-481. https://doi.org/doi.org/10.1021/acs.joc.9b02541
  23. Golden, J. E. (2019). Efficacy of a ML336 Derivative against Venezuelan and Eastern Equine Encephalitis Viruses. Antiviral Research167, 25-34. https://doi.org/10.1016/j.antiviral.2019.04.004
  24. Milanes, J., Suryadi, J., Abendroth, J., Voorhis, W. V., Barrett, K. F., Dranow, D., Phan, I., Patrick, S., Rozema, S., Khalifa, M., Golden, J. E., & Morris, J. (2019). Enzymatic and structural characterization of the Naegleria fowleri glucokinase. Antimicrobial Agents Chemotherotherapy65(5). https://doi.org/10.1128/AAC.02410-18
  25. Golden, J. E. A Novel Compound, ML336, Inhibits VEEV Replication by Interfering with Viral RNA Synthesis. https://doi.org/10.1101/343228
  26. Golden, J. E. (2019). “In This Issue, March” Overview and significance of three highlighted articles featured in the March 2019 issue is summarized. . ACS Med. Chem. Lett. 10(3), 227.
  27. Jaffett, V., Nerurkar, A., Cao, X., Guzei, I., & Golden, J. E. (2019). Telescoped Synthesis of C3-Functionalized (E)-Arylamidines Using Ugi-Mumm and Regiospecific Quinazolinone Rearrangements. Org. Biomol. Chem.17(12), 3118-3128. https://doi.org/10.1039/c9ob00073a
  28. Rinis, N., Golden, J. E., Van Zandt, M. C., Gilmore, R., & Contessa, J. (2018). Editing N-Glycan Site Occupancy With Small Molecule Oligosaccharyltransferase (OST) Inhibitors. Cell Chemical Biology25(10), 1231-1241. https://doi.org/10.1016/j.chembiol.2018.07.005
  29. Yan, G., & Golden, J. E. (2018). Palladium-Catalyzed Cyclocarbonylation of Pyridinylated Vinylogous Amides and Ureas to Generate Ring-Fused Pyridopyrimidinones. Organic Letters20(15), 4393-4396. https://doi.org/10.1021/acs.orglett.8b01275
  30. Flaherty, D., Harris, . T., Schroeder, C. E., Khan, H., Kahney, E., Hackler, A., Patrick, S. L., Weiner, W. S., Aube, J., Sharlow, E. R., Morris, J. C., & Golden, J. E. (2017). Optimization and Evaluation of Antiparasitic Benzamidobenzoic Acids as Inhibitors of Kinetoplastid Hexokinase. Chem Med Chem, 1994-2005. https://doi.org/10.1002/cmdc.201700592
  31. Gordhan, H. M., Milanes, J., Qiu, Y., Golden, J. E., Christensen, K., Morris, J., & Whitehead, D. A. (2017). A Targeted Delivery Strategy for the Development of Potent Trypanocides. Chem Comm53, 8735-8738. https://doi.org/10.1039/C7CC03378H
  32. Hackler, A., Patrick, S. L., Kahney, E. W., Flaherty, D. P., Sharlow, E. R., Morris, J. C., & Golden, J. E. (2017). Antiparasitic lethality of sulfonamidebenzamides in kinetoplastids.. Bioorganic & medicinal chemistry letters27(4), 755-758. https://doi.org/10.1016/j.bmcl.2017.01.043
  33. Adcock, R. S., Chu, Y. K., Golden, J. E., & Chung, D. H. (2017). Evaluation of anti-Zika virus activities of broad-spectrum antivirals and NIH clinical collection compounds using a cell-based, high-throughput screen assay.. Antiviral research138, 47-56. https://doi.org/10.1016/j.antiviral.2016.11.018
  34. Gordhan, H. M., Patrick, S. L., Swasy, M. I., Hackler, A. L., Anayee, M., Golden, J. E., Morris, J. C., & Whitehead, D. C. (2017). Evaluation of substituted ebselen derivatives as potential trypanocidal agents.. Bioorganic & medicinal chemistry letters27(3), 537-541. https://doi.org/10.1016/j.bmcl.2016.12.021
  35. Swingle, M., Volmar, C. H., Saldanha, S. A., Chase, P., Eberhart, C., Salter, E. A., D’Arcy, B., Schroeder, C. E., Golden, J. E., Wierzbicki, A., Hodder, P., & Honkanen, R. E. (2017). An Ultra-High-Throughput Screen for Catalytic Inhibitors of Serine/Threonine Protein Phosphatases Types 1 and 5 (PP1C and PP5C).. SLAS discovery22(1), 21-31. https://doi.org/10.1177/1087057116668852
  36. Lopez-Sambrooks, C., Shrimal, ., Khodier, C., Flaherty, D., Charest, J., Gao, N., Lewis, T. A., Lehrman, M. A., Gilmore, R., Golden, J. E., & Contessa, J. N. (2016). A Small Molecule Inhibitor of the Oligosaccharyltransferase Induces Senescence in Receptor Tyrosine Kinase Dependent Tumors. Nature Chemical Biology12(12), 1023-1030.
  37. Lopez-Sambrooks, C., Shrimal, S., Khodier, C., Flaherty, D. P., Rinis, N., Charest, J. C., Gao, N., Zhao, P., Wells, L., Lewis, T. A., Lehrman, M. A., Gilmore, R., Golden, J. E., & Contessa, J. N. (2016). Oligosaccharyltransferase inhibition induces senescence in RTK-driven tumor cells.. Nature chemical biology12(12), 1023-1030. https://doi.org/10.1038/nchembio.2194
  38. Weisshaar, M., Cox, R., Morehouse, Z., Kyasa, S., Yan, D., Oberacker, P., Mao, S., Golden, J. E., Lowen, A., Natchus, M., & Plemper , R. (2016). Identification and Characterization of Influenza Virus Entry Inhibitors Through Dual-Myxovirus High-Throughput Screening. Journal of Virology90(16), 7368-7387. https://doi.org/10.1128/JVI.00898-16
  39. Chung, D., Golden, J. E., Adcock, R., Schroeder, C. E., Chu, Y., Sotsky, J., Cramer, D., Chilton, P., Song, C., Anantpadma, M., Davey, R., Prodhan, A., Yin, X., & Zhang, X. (2016). Discovery of a broad-spectrum antiviral compound that inhibits pyrimidine biosynthesis and establishes a type 1 interferon-independent antiviral state. Antimicrobial Agents and Chemotherapy60(8), 4552-62. https://doi.org/10.1128/AAC.00282-16
  40. Schroeder, C. E., Neuenswander, S. A., Yao, T., Aubé, J., & Golden, J. E. (2016). One-pot, regiospecific assembly of (E)-benzamidines from δ- and γ-amino acids via an intramolecular aminoquinazolinone rearrangement.. Organic & biomolecular chemistryhttps://doi.org/10.1039/c5ob02378e
  41. Chattopadhyay, D., Swingle, M. R., Salter, E. A., Wood, E., D’Arcy, B., Zivanov, C., Abney, K., Musiyenko, A., Rusin, S. F., Kettenbach, A., Yet, L., Schroeder, C. E., Golden, J. E., Dunham, W. H., Gingras, A. C., Banerjee, S., Forbes, D., Wierzbicki, A., & Honkanen, R. E. (2016). Crystal structures and mutagenesis of PPP-family ser/thr protein phosphatases elucidate the selectivity of cantharidin and novel norcantharidin-based inhibitors of PP5C.. Biochemical pharmacologyhttps://doi.org/10.1016/j.bcp.2016.03.011
  42. Schreiber, S. L., Kotz, J. D., Li , M., Aubé, J., Austin, C. P., Reed, J. C., Rosen, H., White, E. L., Sklar, L. A., Lindsley, C. W., Alexander, B. R., Bittker, J. A., Clemons, P. A., de Souza, A., Foley, M. A., Palmer, M., Shamji, A. F., Wawer, M. J., McManus, O., … Emmitte, K. A. (2015). Advancing Biological Understanding and Therapeutics Discovery with Small-Molecule Probes.. Cell161(6), 1252-65. https://doi.org/10.1016/j.cell.2015.05.023
  43. Matharu, D. S., Flaherty, D. P., Simpson, D. S., Schroeder, C. E., Chung, D., Yan, D., Noah, J. W., Jonsson, C. B., White, E. L., Aubé, J., Plemper, R. K., Severson, W. E., & Golden, J. E. (2014). Optimization of potent and selective quinazolinediones: inhibitors of respiratory syncytial virus that block RNA-dependent RNA-polymerase complex activity.. Journal of medicinal chemistry57(24), 10314-28. https://doi.org/10.1021/jm500902x
  44. Schroeder, C. E., Yao, T., Sotsky, J., Smith, R. A., Roy, S., Chu, Y. K., Guo, H., Tower, N. A., Noah, J. W., McKellip, S., Sosa, M., Rasmussen, L., Smith, L. H., White, E. L., Aubé, J., Jonsson, C. B., Chung, D., & Golden, J. E. (2014). 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.. Journal of medicinal chemistry57(20), 8608-21. https://doi.org/10.1021/jm501203v
  45. Flaherty, D. P., Simpson, D. S., Miller, M., Maki, B. E., Zou, B., Shi, J., Wu, M., McManus, O. B., Aubé, J., Li , M., & Golden, J. E. (2014). Potent and selective inhibitors of the TASK-1 potassium channel through chemical optimization of a bis-amide scaffold.. Bioorganic & medicinal chemistry letters24(16), 3968-73. https://doi.org/10.1016/j.bmcl.2014.06.032
  46. Harris, M. T., Walker, D. M., Drew, M. E., Mitchell, W. G., Dao, K., Schroeder, C. E., Flaherty, D. P., Weiner, W. S., Golden, J. E., & Morris, J. C. (2013). Interrogating a hexokinase-selected small-molecule library for inhibitors of Plasmodium falciparum hexokinase.. Antimicrobial agents and chemotherapy57(8), 3731-7. https://doi.org/10.1128/AAC.00662-13
  47. Hong, L., Kenney, S. R., Phillips, G. K., Simpson, D., Schroeder, C. E., Nöth, J., Romero, E., Golden, J. E., Waller, A., Strouse, J. J., Carter, M., Chigaev, A., Ursu, O., Oprea, T., Hjelle, B., Golden, J. E., Aubé, J., Hudson, L. G., Buranda, T., … Wandinger-Ness, A. (2013). Characterization of a Cdc42 protein inhibitor and its use as a molecular probe.. The Journal of biological chemistry288(12), 8531-43. https://doi.org/10.1074/jbc.M112.435941
  48. Chung, D. H., Moore, B. P., Matharu, D. S., Golden, J. E., Maddox, C., Rasmussen, L., Sosa, M. I., Ananthan, S., White, E. L., Jia, F., Jonsson, C. B., & Severson, W. E. (2013). A cell based high-throughput screening approach for the discovery of new inhibitors of respiratory syncytial virus.. Virology journal10, 19. https://doi.org/10.1186/1743-422X-10-19
  49. Strouse, J. J., Ivnitski-Steele, I., Khawaja, H. M., Perez, D., Ricci, J., Yao, T., Weiner, W. S., Schroeder, C. E., Simpson, D. S., Maki, B. E., Li , K., Golden, J. E., Foutz, T. D., Waller, A., Evangelisti, A. M., Young, S. M., Chavez, S. E., Garcia, M. J., Ursu, O., … Sklar, L. A. (2013). A selective ATP-binding cassette subfamily G member 2 efflux inhibitor revealed via high-throughput flow cytometry.. Journal of biomolecular screening18(1), 26-38. https://doi.org/10.1177/1087057112456875
  50. Moore, B. P., Chung, D. H., Matharu, D. S., Golden, J. E., Maddox, C., Rasmussen, L., Noah, J. W., Sosa, M. I., Ananthan, S., Tower, N. A., White, E. L., Jia, F., Prisinzano, T. E., Aubé, J., Jonsson, C. B., & Severson, W. E. (2012). (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.. Journal of medicinal chemistry55(20), 8582-7. https://doi.org/10.1021/jm300612z
  51. Agola, J. O., Hong, L., Surviladze, Z., Ursu, O., Waller, A., Strouse, J. J., Simpson, D. S., Schroeder, C. E., Oprea, T. I., Golden, J. E., Aubé, J., Buranda, T., Sklar, L. A., & Wandinger-Ness, A. (2012). A competitive nucleotide binding inhibitor: in vitro characterization of Rab7 GTPase inhibition.. ACS chemical biology7(6), 1095-108. https://doi.org/10.1021/cb3001099
  52. Chen, J., Young, S. M., Allen, C., Seeber, A., Péli-Gulli, M. P., Panchaud, N., Waller, A., Ursu, O., Yao, T., Golden, J. E., Strouse, J. J., Carter, M. B., Kang, H., Bologa, C. G., Foutz, T. D., Edwards, B. S., Peterson, B. R., Aubé, J., Werner-Washburne, M., … Sklar, L. A. (2012). Identification of a small molecule yeast TORC1 inhibitor with a multiplex screen based on flow cytometry.. ACS chemical biology7(4), 715-22. https://doi.org/10.1021/cb200452r
  53. Seguin, S. P., Evans, C. W., Nebane-Akah, M., McKellip, S., Ananthan, S., Tower, N. A., Sosa, M., Rasmussen, L., White, E. L., Maki, B. E., Matharu, D. S., Golden, J. E., Aubé, J., Brodsky, J. L., & Noah, J. W. (2012). High-throughput screening identifies a bisphenol inhibitor of SV40 large T antigen ATPase activity.. Journal of biomolecular screening17(2), 194-203. https://doi.org/10.1177/1087057111421630
  54. Frohn, M., Cee, V. J., Lanman, B. A., Pickrell, A. J., Golden, J. E., Rivenzon-Segal, D., Middleton, S., Fiorino, M., Xu, H., Schrag, M., Xu, Y., McElvain, M., Muller, K., Siu, J., & Bürli, R. (2012). Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: potent S1P₁ agonists with in vivo lymphocyte-depleting activity.. Bioorganic & medicinal chemistry letters22(1), 628-33. https://doi.org/10.1016/j.bmcl.2011.10.069
  55. Golden, J. E., Sanders, S. D., Muller, K. M., & Bürli, R. W. (2008). Modulating N- versus O-arylation in pyrazolone-aryl halide couplings . Tetrahedron Letters 49(5), 794 – 798. https://doi.org/http://dx.doi.org/10.1016/j.tetlet.2007.11.185
  56. Frohn, M., Viswanadhan, V., Pickrell, A. J., Golden, J. E., Muller, K. M., Bürli, R. W., Biddlecome, G., Yoder, S. C., Rogers, N., Dao, J. H., Hungate, R., & Allen, J. R. (2008). Structure-guided design of substituted aza-benzimidazoles as potent hypoxia inducible factor-1alpha prolyl hydroxylase-2 inhibitors.. Bioorganic & medicinal chemistry letters18(18), 5023-6. https://doi.org/10.1016/j.bmcl.2008.08.012
  57. Frankowski, K. J., Golden, J. E., Zeng, Y., Lei, Y., & Aubé, J. (2008). Syntheses of the Stemona alkaloids (+/-)-stenine, (+/-)-neostenine, and (+/-)-13-epineostenine using a stereodivergent Diels-Alder/azido-Schmidt reaction.. Journal of the American Chemical Society130(18), 6018-24. https://doi.org/10.1021/ja800574m
  58. Bürli, R. W., Xu, H., Zou, X., Muller, K., Golden, J. E., Frohn, M., Adlam, M., Plant, M. H., Wong, M., McElvain, M., Regal, K., Viswanadhan, V. N., Tagari, P., & Hungate, R. (2006). Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents.. Bioorganic & medicinal chemistry letters16(14), 3713-8. https://doi.org/10.1016/j.bmcl.2006.04.068
  59. Golden, J. E., & Aubé, J. (2002). A combined intramolecular Diels-Alder/intramolecular schmidt reaction: formal synthesis of (+/-)-stenine.. Angewandte Chemie (International ed. in English)41(22), 4316-8. https://doi.org/10.1002/1521-3773(20021115)41:22<4316::AID-ANIE4316>3.0.CO;2-U