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.
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 & Catalysis, 365, 4567. https://doi.org/10.1002/adsc.202300994
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
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
Ogorek, T., & Golden, J. E. (2023). Advances in the Development of Small Molecule Antivirals Against Equine Encephalitic Alphaviruses.. Viruses. https://doi.org/org/10.3390/v15020413
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 Chem, 87(21), 14889-14898.
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.
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 Lett, 13(4), 546-553.
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
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
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.
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.
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. Virol, 50, 1-7. https://doi.org/10.1016/j.coviro.2021.06.008
Golden, J. E. (2020). Dual Stage Picolinic Acid Derived Inhibitors of Toxoplasma gondii. ACS Med. Chem. Lett. , 11(12), 2382-2388.
Golden, J. E. (2020). Emergence and magnitude of ML336 resistance in Venezuelan equine encephalitis virus depends on the microenvironment. J. Virology. https://doi.org/10.1128/JVI.00317-20.
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 Journal, 26, 2486-2492. https://doi.org/10.1002/chem.201905219
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
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 Res. https://doi.org/doi: 10.1016/j.antiviral.2019.104674.
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. Chem, 85(2), 464-481. https://doi.org/doi.org/10.1021/acs.joc.9b02541
Golden, J. E. (2019). Efficacy of a ML336 Derivative against Venezuelan and Eastern Equine Encephalitis Viruses. Antiviral Research, 167, 25-34. https://doi.org/10.1016/j.antiviral.2019.04.004
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 Chemotherotherapy, 65(5). https://doi.org/10.1128/AAC.02410-18
Golden, J. E. A Novel Compound, ML336, Inhibits VEEV Replication by Interfering with Viral RNA Synthesis. https://doi.org/10.1101/343228
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.
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
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 Biology, 25(10), 1231-1241. https://doi.org/10.1016/j.chembiol.2018.07.005
Yan, G., & Golden, J. E. (2018). Palladium-Catalyzed Cyclocarbonylation of Pyridinylated Vinylogous Amides and Ureas to Generate Ring-Fused Pyridopyrimidinones. Organic Letters, 20(15), 4393-4396. https://doi.org/10.1021/acs.orglett.8b01275
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
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 Comm, 53, 8735-8738. https://doi.org/10.1039/C7CC03378H
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 letters, 27(4), 755-758. https://doi.org/10.1016/j.bmcl.2017.01.043
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 research, 138, 47-56. https://doi.org/10.1016/j.antiviral.2016.11.018
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 letters, 27(3), 537-541. https://doi.org/10.1016/j.bmcl.2016.12.021
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 discovery, 22(1), 21-31. https://doi.org/10.1177/1087057116668852
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 Biology, 12(12), 1023-1030.
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 biology, 12(12), 1023-1030. https://doi.org/10.1038/nchembio.2194
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 Virology, 90(16), 7368-7387. https://doi.org/10.1128/JVI.00898-16
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 Chemotherapy, 60(8), 4552-62. https://doi.org/10.1128/AAC.00282-16
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 chemistry. https://doi.org/10.1039/c5ob02378e
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 pharmacology. https://doi.org/10.1016/j.bcp.2016.03.011
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.. Cell, 161(6), 1252-65. https://doi.org/10.1016/j.cell.2015.05.023
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 chemistry, 57(24), 10314-28. https://doi.org/10.1021/jm500902x
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 chemistry, 57(20), 8608-21. https://doi.org/10.1021/jm501203v
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 letters, 24(16), 3968-73. https://doi.org/10.1016/j.bmcl.2014.06.032
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 chemotherapy, 57(8), 3731-7. https://doi.org/10.1128/AAC.00662-13
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 chemistry, 288(12), 8531-43. https://doi.org/10.1074/jbc.M112.435941
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 journal, 10, 19. https://doi.org/10.1186/1743-422X-10-19
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 screening, 18(1), 26-38. https://doi.org/10.1177/1087057112456875
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 chemistry, 55(20), 8582-7. https://doi.org/10.1021/jm300612z
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 biology, 7(6), 1095-108. https://doi.org/10.1021/cb3001099
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 biology, 7(4), 715-22. https://doi.org/10.1021/cb200452r
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 screening, 17(2), 194-203. https://doi.org/10.1177/1087057111421630
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 letters, 22(1), 628-33. https://doi.org/10.1016/j.bmcl.2011.10.069
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 letters, 18(18), 5023-6. https://doi.org/10.1016/j.bmcl.2008.08.012
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 Society, 130(18), 6018-24. https://doi.org/10.1021/ja800574m
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 letters, 16(14), 3713-8. https://doi.org/10.1016/j.bmcl.2006.04.068