2025
Kowalczyk ET, Medubi KM, Meyer MJ, Toriola MA, Haasch TJ, Vesperman MR, Webb DA, Stafford DC, Yocum GT, Emala CW, Arnold LA. Development of novel pegylated imidazobenzodiazepines as inhaled asthma drug candidates. Respir Med. 2025 Oct 22:108449. doi: 10.1016/j.rmed.2025.108449. Epub ahead of print. PMID: 41135912.
Fernando MRT, Vincent AB, Harrington SG, Toriola MA, Medubi KM, Meyer MJ, Webb DA, Arnold LA. Development of novel alpha 2B adrenergic receptor ligands by using a palladium catalyzed Buchwald Hartwig amination with a brominated benzodiazepine. RSC Med Chem. 2025 Sep 16;. doi: 10.1039/d5md00611b. [Epub ahead of print] PubMed PMID: 41049791; PubMed Central PMCID: PMC12495306.
Toriola MA, Timlin E, Bulbule S, Reyes A, Adedeji OM, Gottschalk CG, Barua A, Arnold LA, Roy A. Genetic depletion of early autophagy protein ATG13 impairs mitochondrial energy metabolism, augments oxidative stress, induces the polarization of macrophages to M1 inflammatory mode, and compromises myelin integrity in skeletal muscle. Res Sq. 2025 Aug 6;. doi: 10.21203/rs.3.rs-7189456/v1. PubMed PMID: 40799759; PubMed Central PMCID: PMC12340908.
Rahman AFMT, Benko A, Bulbule S, Gottschalk CG, Arnold LA, Roy A. Tetrahydrobiopterin in Myalgic Encephalomyelitis/Chronic Fatigue Syndrome: A Friend or Foe?. Biomolecules. 2025 Jan 10;15(1). doi: 10.3390/biom15010102. Review. PubMed PMID: 39858496; PubMed Central PMCID: PMC11763651.
Drosen ME, Bulbule S, Gottschalk G, Peterson D, Allen LA, Arnold LA, Roy A. Inactivation of ATG13 stimulates chronic demyelinating pathologies in muscle-serving nerves and spinal cord. Immunol Res. 2025 Jan 7;73(1):27. doi: 10.1007/s12026-024-09557-7. PubMed PMID: 39777574; PubMed Central PMCID: PMC11706859.
2024
Rahman AFMT, Bulbule S, Belayet JB, Benko A, Gottschalk CG, Frick DN, Arnold LA, Hossain MM, Roy A. JRM-28, a Novel HDAC2 Inhibitor, Upregulates Plasticity-Associated Proteins in Hippocampal Neurons and Enhances Morphological Plasticity via Activation of CREB: Implications for Alzheimer’s Disease. Cells. 2024 Nov 27;13(23). doi: 10.3390/cells13231964. PubMed PMID: 39682714; PubMed Central PMCID: PMC11640089.
Bulbule S, Gottschalk CG, Drosen ME, Peterson D, Arnold LA, Roy A. Dysregulation of tetrahydrobiopterin metabolism in myalgic encephalomyelitis/chronic fatigue syndrome by pentose phosphate pathway. J Cent Nerv Syst Dis. 2024;16:11795735241271675. doi: 10.1177/11795735241271675. eCollection 2024. PubMed PMID: 39161795; PubMed Central PMCID: PMC11331476.
Qian J, Yu F, Arnold LA, Saha A, Zheng L, Zhao M. Exploring structural features of sleep-enhancing peptides derived from casein hydrolysates by chemometrics and random forest methodology. Food Chem. 2024 Dec 15;461:140838. doi: 10.1016/j.foodchem.2024.140838. Epub 2024 Aug 10. PubMed PMID: 39167944.
Sharmin D, Divović B, Ping X, Cerne R, Smith JL, Rezvanian S, Mondal P, Meyer MJ, Kiley ME, Arnold LA, Mian MY, Pandey KP, Jin X, Mitrović JR, Djorović D, Lippa A, Cook JM, Golani LK, Scholze P, Savić MM, Witkin JM. New Imidazodiazepine Analogue, 5-(8-Bromo-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole, Provides a Simplified Synthetic Scheme, High Oral Plasma and Brain Exposures, and Produces Antiseizure Efficacy in Mice, and Antiepileptogenic Activity in Neural Networks in Brain Slices from a Patient with Mesial Temporal Lobe Epilepsy. ACS Chem Neurosci. 2024 Feb 7;15(3):517-526. doi: 10.1021/acschemneuro.3c00555. Epub 2024 Jan 4. PubMed PMID: 38175916.
Rajaratnam V, Islam MM, Kub EF, Rajaratnam S, Kim KB, Rahman MT, Rashid F, Benko AM, Cook JM, Arnold LA, Mirza SP. Development and validation of an LC-MS/MS method for the determination of ARN14988, an acid ceramidase inhibitor, and its application to a pharmacokinetic study in a mouse model. Biomed Chromatogr. 2024 Jan;38(1):e5754. doi: 10.1002/bmc.5754. Epub 2023 Sep 26. PubMed PMID: 37750452.
2023
Webb DA, Alsudani Z, Xu G, Gao P, Arnold LA. Improved 2-pyridyl reductive homocoupling reaction using biorenewable solvent Cyrene™ (dihydrolevoglucosenone). RSC Sustain. 2023 Sep 7;1(6):1522-1529. doi: 10.1039/d3su00005b. eCollection 2023 Sep 7. PubMed PMID: 38013944; PubMed Central PMCID: PMC10484179.
Webb DA, Meyer MJ, Medubi KM, Tylek AS, Yocum GT, Roni MSR, Zahn NM, Swartwout SA, Masoud AK, Emala CW, Stafford DC, Arnold LA. Design, Synthesis, and Biological Evaluation of Novel Spiro Imidazobenzodiazepines to Identify Improved Inhaled Bronchodilators. J Med Chem. 2023 Jul 27;66(14):9853-9865. doi: 10.1021/acs.jmedchem.3c00647. Epub 2023 Jul 7. PubMed PMID: 37418196; PubMed Central PMCID: PMC10833105.
Ping X, Meyer MJ, Zahn NM, Golani LK, Sharmin D, Pandey KP, Revanian S, Mondal P, Jin X, Arnold LA, Cerne R, Cook JM, Divović B, Savić MM, Lippa A, Smith JL, Witkin JM. Comparative anticonvulsant activity of the GABAkine KRM-II-81 and a deuterated analog. Drug Dev Res. 2023 May;84(3):527-531. doi: 10.1002/ddr.22042. Epub 2023 Feb 7. PubMed PMID: 36748904.
Pandey KP, Divović B, Rashid F, Golani LK, Cerne R, Zahn NM, Meyer MJ, Arnold LA, Sharmin D, Mian MY, Smith JL, Ping X, Jin X, Lippa A, Tiruveedhula VVNPB, Cook JM, Savić MM, Witkin JM. Structural Analogs of the GABAkine KRM-II-81 Are Orally Bioavailable Anticonvulsants without Sedation. J Pharmacol Exp Ther. 2023 Apr;385(1):50-61. doi: 10.1124/jpet.122.001362. Epub 2023 Feb 6. PubMed PMID: 36746611; PubMed Central PMCID: PMC10029819.
Johnston N, Samuels TL, Goetz CJ, Arnold LA, Smith BC, Seabloom D, Wuertz B, Ondrey F, Wiedmann TS, Vuksanovic N, Silvaggi NR, MacKinnon AC, Miller J, Bock J, Blumin JH. Oral and Inhaled Fosamprenavir Reverses Pepsin-Induced Damage in a Laryngopharyngeal Reflux Mouse Model. Laryngoscope. 2023 Jan;133 Suppl 1(Suppl 1):S1-S11. doi: 10.1002/lary.30242. Epub 2022 Jun 9. PubMed PMID: 35678265; PubMed Central PMCID: PMC9732152.
2022
Perez-Zoghbi JF, Sajorda DR, Webb DA, Arnold LA, Emala CW, Yocum GT. Imidazobenzodiazepine PI320 Relaxes Mouse Peripheral Airways by Inhibiting Calcium Mobilization. Am J Respir Cell Mol Biol. 2022 Oct;67(4):482-490. doi: 10.1165/rcmb.2022-0084OC. PubMed PMID: 35776523; PubMed Central PMCID: PMC9564932.
Khazan N, Kim KK, Hansen JN, Singh NA, Moore T, Snyder CWA, Pandita R, Strawderman M, Fujihara M, Takamura Y, Jian Y, Battaglia N, Yano N, Teramoto Y, Arnold LA, Hopson R, Kishor K, Nayak S, Ojha D, Sharon A, Ashton JM, Wang J, Milano MT, Miyamoto H, Linehan DC, Gerber SA, Kawar N, Singh AP, Tabdanov ED, Dokholyan NV, Kakuta H, Jurutka PW, Schor NF, Rowswell-Turner RB, Singh RK, Moore RG. Identification of a Vitamin-D Receptor Antagonist, MeTC7, which Inhibits the Growth of Xenograft and Transgenic Tumors In Vivo. J Med Chem. 2022 Apr 28;65(8):6039-6055. doi: 10.1021/acs.jmedchem.1c01878. Epub 2022 Apr 11. PubMed PMID: 35404047; PubMed Central PMCID: PMC9059124.
Golani LK, Divović B, Sharmin D, Pandey KP, Mian MY, Cerne R, Zahn NM, Meyer MJ, Tiruveedhula VVNPB, Smith JL, Ping X, Jin X, Lippa A, Schkeryantz JM, Arnold LA, Cook JM, Savić MM, Witkin JM. Metabolism, pharmacokinetics, and anticonvulsant activity of a deuterated analog of the α2/3-selective GABAkine KRM-II-81. Biopharm Drug Dispos. 2022 Apr;43(2):66-75. doi: 10.1002/bdd.2313. Epub 2022 Mar 10. PubMed PMID: 35194800.
Rashid Roni MS, Zahn NM, Yocum GT, Webb DA, Mian MY, Meyer MJ, Tylek AS, Cook JM, Emala CW, Stafford DC, Arnold LA. Comparative pharmacodynamic and pharmacokinetic study of MIDD0301 and its (S) enantiomer. Drug Dev Res. 2022 Jun;83(4):979-992. doi: 10.1002/ddr.21926. Epub 2022 Mar 4. PubMed PMID: 35246861; PubMed Central PMCID: PMC9246881.
Belayet JB, Beamish S, Rahaman M, Alanani S, Virdi RS, Frick DN, Rahman AFMT, Ulicki JS, Biswas S, Arnold LA, Roni MSR, Cheng EY, Steeber DA, Frick KM, Hossain MM. Development of a Novel, Small-Molecule Brain-Penetrant Histone Deacetylase Inhibitor That Enhances Spatial Memory Formation in Mice. J Med Chem. 2022 Feb 24;65(4):3388-3403. doi: 10.1021/acs.jmedchem.1c01928. Epub 2022 Feb 8. PubMed PMID: 35133171; PubMed Central PMCID: PMC9135144.
Zahn NM, Roni MSR, Yocum GT, Meyer MJ, Webb DA, Mian MY, Cook JM, Stafford DC, Emala CW, Arnold LA. Development of Inhaled GABA(A) Receptor Modulators to Improve Airway Function in Bronchoconstrictive Disorders. ACS Pharmacol Transl Sci. 2022 Feb 11;5(2):80-88. doi: 10.1021/acsptsci.1c00238. eCollection 2022 Feb 11. PubMed PMID: 35187417; PubMed Central PMCID: PMC8844962.
2021
Roni MSR, Zahn NM, Mikulsky BN, Webb DA, Mian MY, Knutson DE, Guthrie ML, Cook JM, Stafford DC, Arnold LA. Identification and Quantification of MIDD0301 Metabolites. Curr Drug Metab. 2021;22(14):1114-1123. doi: 10.2174/1389200222666211202093841. PubMed PMID: 34856893; PubMed Central PMCID: PMC8760168.
Yu OB, Webb DA, Di Milo ES, Mutchie TR, Teske KA, Chen T, Lin W, Peluso-Iltis C, Rochel N, Helmstädter M, Merk D, Arnold LA. Biological evaluation and synthesis of calcitroic acid. Bioorg Chem. 2021 Nov;116:105310. doi: 10.1016/j.bioorg.2021.105310. Epub 2021 Aug 28. Review. PubMed PMID: 34482171; PubMed Central PMCID: PMC8592288.
Fan H, Zaman MAU, Chen W, Ali T, Campbell A, Zhang Q, Setu NI, Saxon E, Zahn NM, Benko AM, Arnold LA, Peng X. Assessment of Phenylboronic Acid Nitrogen Mustards as Potent and Selective Drug Candidates for Triple-Negative Breast Cancer. ACS Pharmacol Transl Sci. 2021 Apr 9;4(2):687-702. doi: 10.1021/acsptsci.0c00092. eCollection 2021 Apr 9. PubMed PMID: 33860194; PubMed Central PMCID: PMC8033613.
2020
Zahn NM, Mikulsky BN, Roni MSR, Yocum GT, Mian MY, Knutson DE, Cook JM, Emala CW, Stafford DC, Arnold LA. Nebulized MIDD0301 Reduces Airway Hyperresponsiveness in Moderate and Severe Murine Asthma Models. ACS Pharmacol Transl Sci. 2020 Dec 11;3(6):1381-1390. doi: 10.1021/acsptsci.0c00180. eCollection 2020 Dec 11. PubMed PMID: 33344908; PubMed Central PMCID: PMC7737320.
Pandey KP, Khan ZA, Golani LK, Mondal P, Mian Y, Rashid F, Tiruveedhula VVNPB, Knutson DE, Sharmin D, Ahmed T, Rezvanian S, Zahn NM, Arnold LA, Witkin JM, Cook JM. Design, synthesis and characterization of novel gamma‑aminobutyric acid type A receptor ligands. ARKIVOC. 2020;2020(Pt 7):242-256. doi: 10.24820/ark.5550190.p011.398. Epub 2020 Dec 2. PubMed PMID: 33642954; PubMed Central PMCID: PMC7909486.
Li G, Nieman AN, Mian MY, Zahn NM, Mikulsky BN, Poe MM, Methuku KR, Liu Y, Cook JM, Stafford DC, Arnold LA. A Structure-Activity Relationship Comparison of Imidazodiazepines Binding at Kappa, Mu, and Delta Opioid Receptors and the GABA(A) Receptor. Molecules. 2020 Aug 25;25(17). doi: 10.3390/molecules25173864. PubMed PMID: 32854311; PubMed Central PMCID: PMC7503500.
Knutson DE, Roni R, Mian Y, Cook JM, Stafford DC, Arnold LA. Improved scale-up synthesis and purification of clinical asthma candidate MIDD0301. Org Process Res Dev. 2020 Aug 21;24(8):1467-1476. doi: 10.1021/acs.oprd.0c00200. Epub 2020 Jul 29. PubMed PMID: 32952391; PubMed Central PMCID: PMC7497793.
Nieman AN, Li G, Zahn NM, Mian MY, Mikulsky BN, Hoffman DA, Wilcox TM, Kehoe AS, Luecke IW, Poe MM, Alvarez-Carbonell D, Cook JM, Stafford DC, Arnold LA. Targeting Nitric Oxide Production in Microglia with Novel Imidazodiazepines for Nonsedative Pain Treatment. ACS Chem Neurosci. 2020 Jul 1;11(13):2019-2030. doi: 10.1021/acschemneuro.0c00324. Epub 2020 Jun 18. PubMed PMID: 32511908; PubMed Central PMCID: PMC7380323.
Roni MSR, Li G, Mikulsky BN, Knutson DE, Mian MY, Zahn NM, Cook JM, Stafford DC, Arnold LA. The Effects of pH on the Structure and Bioavailability of Imidazobenzodiazepine-3-Carboxylate MIDD0301. Mol Pharm. 2020 Apr 6;17(4):1182-1192. doi: 10.1021/acs.molpharmaceut.9b01210. Epub 2020 Feb 26. PubMed PMID: 32069056; PubMed Central PMCID: PMC7216793.
Yu OB, Mutchie TR, Di Milo ES, Arnold LA. Synthesis and biological evaluation of calcioic acid. Steroids. 2020 Feb;154:108536. doi: 10.1016/j.steroids.2019.108536. Epub 2019 Nov 6. PubMed PMID: 31704333; PubMed Central PMCID: PMC6980330.
2019
Porter JD, Vivas O, Weaver CD, Alsafran A, DiMilo E, Arnold LA, Dickson EJ, Dockendorff C. An anthrone-based Kv7.2/7.3 channel blocker with improved properties for the investigation of psychiatric and neurodegenerative disorders. Bioorg Med Chem Lett. 2019 Dec 1;29(23):126681. doi: 10.1016/j.bmcl.2019.126681. Epub 2019 Sep 14. PubMed PMID: 31668424; PubMed Central PMCID: PMC6858848.
Gandhi DM, Rosas R Jr, Greve E, Kentala K, D-R Diby N, Snyder VA, Stephans A, Yeung THW, Subramaniam S, DiMilo E, Kurtenbach KE, Arnold LA, Weiler H, Dockendorff C. The parmodulin NRD-21 is an allosteric inhibitor of PAR1 Gq signaling with improved anti-inflammatory activity and stability. Bioorg Med Chem. 2019 Sep 1;27(17):3788-3796. doi: 10.1016/j.bmc.2019.06.043. Epub 2019 Jun 29. PubMed PMID: 31320211; PubMed Central PMCID: PMC6706283.
Zahn NM, Huber AT, Mikulsky BN, Stepanski ME, Kehoe AS, Li G, Schussman M, Rashid Roni MS, Kodali R, Cook JM, Stafford DC, Steeber DA, Arnold LA. MIDD0301 – A first-in-class anti-inflammatory asthma drug targets GABA(A) receptors without causing systemic immune suppression. Basic Clin Pharmacol Toxicol. 2019 Jul;125(1):75-84. doi: 10.1111/bcpt.13206. Epub 2019 Feb 21. PubMed PMID: 30694594; PubMed Central PMCID: PMC6565495.
Prevot TD, Li G, Vidojevic A, Misquitta KA, Fee C, Santrac A, Knutson DE, Stephen MR, Kodali R, Zahn NM, Arnold LA, Scholze P, Fisher JL, Marković BD, Banasr M, Cook JM, Savic M, Sibille E. Novel Benzodiazepine-Like Ligands with Various Anxiolytic, Antidepressant, or Pro-Cognitive Profiles. Mol Neuropsychiatry. 2019 Apr;5(2):84-97. doi: 10.1159/000496086. Epub 2019 Jan 23. PubMed PMID: 31192221; PubMed Central PMCID: PMC6528097.
Mutchie TR, Yu OB, Di Milo ES, Arnold LA. Alternative binding sites at the vitamin D receptor and their ligands. Mol Cell Endocrinol. 2019 Apr 5;485:1-8. doi: 10.1016/j.mce.2019.01.011. Epub 2019 Jan 14. Review. PubMed PMID: 30654005; PubMed Central PMCID: PMC6444937.
Majewski MW, Gandhi DM, Rosas R Jr, Kodali R, Arnold LA, Dockendorff C. Design and Evaluation of Heterobivalent PAR1-PAR2 Ligands as Antagonists of Calcium Mobilization. ACS Med Chem Lett. 2019 Jan 10;10(1):121-126. doi: 10.1021/acsmedchemlett.8b00538. eCollection 2019 Jan 10. PubMed PMID: 30655958; PubMed Central PMCID: PMC6331166.
Yocum GT, Perez-Zoghbi JF, Danielsson J, Kuforiji AS, Zhang Y, Li G, Rashid Roni MS, Kodali R, Stafford DC, Arnold LA, Cook JM, Emala CW Sr. A novel GABA(A) receptor ligand MIDD0301 with limited blood-brain barrier penetration relaxes airway smooth muscle ex vivo and in vivo. Am J Physiol Lung Cell Mol Physiol. 2019 Feb 1;316(2):L385-L390. doi: 10.1152/ajplung.00356.2018. Epub 2018 Nov 29. PubMed PMID: 30489155; PubMed Central PMCID: PMC6397346.
2018
Chen W, Fan H, Balakrishnan K, Wang Y, Sun H, Fan Y, Gandhi V, Arnold LA, Peng X. Discovery and Optimization of Novel Hydrogen Peroxide Activated Aromatic Nitrogen Mustard Derivatives as Highly Potent Anticancer Agents. J Med Chem. 2018 Oct 25;61(20):9132-9145. doi: 10.1021/acs.jmedchem.8b00559. Epub 2018 Oct 10. PubMed PMID: 30247905.
Li G, Golani LK, Jahan R, Rashid F, Cook JM. Improved Synthesis of Anxiolytic, Anticonvulsant and Antinociceptive α2/α3-GABA(A)ergic Receptor Subtype Selective Ligands as Promising Agents to Treat Anxiety, Epilepsy, as well as Neuropathic Pain. Synthesis (Stuttg). 2018 Oct;50(20):4124-4132. doi: 10.1055/s-0037-1610211. PubMed PMID: 32773890; PubMed Central PMCID: PMC7413181.
Wyatt BN, Arnold LA, St Maurice M. A high-throughput screening assay for pyruvate carboxylase. Anal Biochem. 2018 Jun 1;550:90-98. doi: 10.1016/j.ab.2018.04.012. Epub 2018 Apr 12. PubMed PMID: 29655770.
Forkuo GS, Nieman AN, Kodali R, Zahn NM, Li G, Rashid Roni MS, Stephen MR, Harris TW, Jahan R, Guthrie ML, Yu OB, Fisher JL, Yocum GT, Emala CW, Steeber DA, Stafford DC, Cook JM, Arnold LA. A Novel Orally Available Asthma Drug Candidate That Reduces Smooth Muscle Constriction and Inflammation by Targeting GABA(A) Receptors in the Lung. Mol Pharm. 2018 May 7;15(5):1766-1777. doi: 10.1021/acs.molpharmaceut.7b01013. Epub 2018 Apr 2. PubMed PMID: 29578347; PubMed Central PMCID: PMC5954213.
Li G, Stephen MR, Kodali R, Zahn NM, Poe MM, Tiruveedhula VVNPB, Huber AT, Schussman MK, Qualmann K, Panhans CM, Raddatz NJ, Baker DA, Prevot TD, Banasr M, Sibille E, Arnold LA, Cook JM. Synthesis of chiral GABA(A) receptor subtype selective ligands as potential agents to treat schizophrenia as well as depression. ARKIVOC. 2018;2018(4):158-182. doi: 10.24820/ark.5550190.p010.460. Epub 2018 Mar 11. PubMed PMID: 32774192; PubMed Central PMCID: PMC7413308.
Knutson DE, Kodali R, Divović B, Treven M, Stephen MR, Zahn NM, Dobričić V, Huber AT, Meirelles MA, Verma RS, Wimmer L, Witzigmann C, Arnold LA, Chiou LC, Ernst M, Mihovilovic MD, Savić MM, Sieghart W, Cook JM. Design and Synthesis of Novel Deuterated Ligands Functionally Selective for the γ-Aminobutyric Acid Type A Receptor (GABA(A)R) α6 Subtype with Improved Metabolic Stability and Enhanced Bioavailability. J Med Chem. 2018 Mar 22;61(6):2422-2446. doi: 10.1021/acs.jmedchem.7b01664. Epub 2018 Mar 6. PubMed PMID: 29481759; PubMed Central PMCID: PMC6941172.
Teske KA, Bogart JW, Arnold LA. Novel VDR antagonists based on the GW0742 scaffold. Bioorg Med Chem Lett. 2018 Feb 1;28(3):351-354. doi: 10.1016/j.bmcl.2017.12.041. Epub 2017 Dec 19. PubMed PMID: 29287957; PubMed Central PMCID: PMC6008168.
McMurray KMJ, Ramaker MJ, Barkley-Levenson AM, Sidhu PS, Elkin PK, Reddy MK, Guthrie ML, Cook JM, Rawal VH, Arnold LA, Dulawa SC, Palmer AA. Identification of a novel, fast-acting GABAergic antidepressant. Mol Psychiatry. 2018 Feb;23(2):384-391. doi: 10.1038/mp.2017.14. Epub 2017 Mar 21. PubMed PMID: 28322281; PubMed Central PMCID: PMC5608625.
2017
Teske KA, Rai G, Nandhikonda P, Sidhu PS, Feleke B, Simeonov A, Yasgar A, Jadhav A, Maloney DJ, Arnold LA. Parallel Chemistry Approach to Identify Novel Nuclear Receptor Ligands Based on the GW0742 Scaffold. ACS Comb Sci. 2017 Oct 9;19(10):646-656. doi: 10.1021/acscombsci.7b00066. Epub 2017 Sep 5. PubMed PMID: 28825467; PubMed Central PMCID: PMC5643073.
Forkuo GS, Nieman AN, Yuan NY, Kodali R, Yu OB, Zahn NM, Jahan R, Li G, Stephen MR, Guthrie ML, Poe MM, Hartzler BD, Harris TW, Yocum GT, Emala CW, Steeber DA, Stafford DC, Cook JM, Arnold LA. Alleviation of Multiple Asthmatic Pathologic Features with Orally Available and Subtype Selective GABA(A) Receptor Modulators. Mol Pharm. 2017 Jun 5;14(6):2088-2098. doi: 10.1021/acs.molpharmaceut.7b00183. Epub 2017 May 1. PubMed PMID: 28440659; PubMed Central PMCID: PMC5497587.
Witkin JM, Cerne R, Wakulchik M, S J, Gleason SD, Jones TM, Li G, Arnold LA, Li JX, Schkeryantz JM, Methuku KR, Cook JM, Poe MM. Further evaluation of the potential anxiolytic activity of imidazo[1,5-a][1,4]diazepin agents selective for α2/3-containing GABA(A) receptors. Pharmacol Biochem Behav. 2017 Jun;157:35-40. doi: 10.1016/j.pbb.2017.04.009. Epub 2017 Apr 22. PubMed PMID: 28442369; PubMed Central PMCID: PMC5519285.
Wang Y, Fan H, Balakrishnan K, Lin Z, Cao S, Chen W, Fan Y, Guthrie QA, Sun H, Teske KA, Gandhi V, Arnold LA, Peng X. Hydrogen peroxide activated quinone methide precursors with enhanced DNA cross-linking capability and cytotoxicity towards cancer cells. Eur J Med Chem. 2017 Jun 16;133:197-207. doi: 10.1016/j.ejmech.2017.03.041. Epub 2017 Mar 24. PubMed PMID: 28388522; PubMed Central PMCID: PMC5652303.
Fischer BD, Schlitt RJ, Hamade BZ, Rehman S, Ernst M, Poe MM, Li G, Kodali R, Arnold LA, Cook JM. Pharmacological and antihyperalgesic properties of the novel α2/3 preferring GABA(A) receptor ligand MP-III-024. Brain Res Bull. 2017 May;131:62-69. doi: 10.1016/j.brainresbull.2017.03.001. Epub 2017 Mar 4. PubMed PMID: 28267561; PubMed Central PMCID: PMC5501353.
Jahan R, Stephen MR, Forkuo GS, Kodali R, Guthrie ML, Nieman AN, Yuan NY, Zahn NM, Poe MM, Li G, Yu OB, Yocum GT, Emala CW, Stafford DC, Cook JM, Arnold LA. Optimization of substituted imidazobenzodiazepines as novel asthma treatments. Eur J Med Chem. 2017 Jan 27;126:550-560. doi: 10.1016/j.ejmech.2016.11.045. Epub 2016 Nov 24. PubMed PMID: 27915170; PubMed Central PMCID: PMC5253108.
McMurray KM, Sidhu PS, Cook JM, Arnold LA, Palmer AA. Genetic and pharmacological manipulation of glyoxalase 1 regulates voluntary ethanol consumption in mice. Addict Biol. 2017 Mar;22(2):381-389. doi: 10.1111/adb.12333. Epub 2015 Dec 22. PubMed PMID: 26691867; PubMed Central PMCID: PMC4917470.
2016
Poe MM, Methuku KR, Li G, Verma AR, Teske KA, Stafford DC, Arnold LA, Cramer JW, Jones TM, Cerne R, Krambis MJ, Witkin JM, Jambrina E, Rehman S, Ernst M, Cook JM, Schkeryantz JM. Synthesis and Characterization of a Novel γ-Aminobutyric Acid Type A (GABA(A)) Receptor Ligand That Combines Outstanding Metabolic Stability, Pharmacokinetics, and Anxiolytic Efficacy. J Med Chem. 2016 Dec 8;59(23):10800-10806. doi: 10.1021/acs.jmedchem.6b01332. Epub 2016 Nov 28. PubMed PMID: 27933953; PubMed Central PMCID: PMC5215686.
Yu OB, Arnold LA. Calcitroic Acid-A Review. ACS Chem Biol. 2016 Oct 21;11(10):2665-2672. doi: 10.1021/acschembio.6b00569. Epub 2016 Sep 6. Review. PubMed PMID: 27574921; PubMed Central PMCID: PMC5074857.
Yuan NY, Poe MM, Witzigmann C, Cook JM, Stafford D, Arnold LA. Characterization of GABA(A) receptor ligands with automated patch-clamp using human neurons derived from pluripotent stem cells. J Pharmacol Toxicol Methods. 2016 Nov-Dec;82:109-114. doi: 10.1016/j.vascn.2016.08.006. Epub 2016 Aug 18. PubMed PMID: 27544543; PubMed Central PMCID: PMC5116268.
Forkuo GS, Guthrie ML, Yuan NY, Nieman AN, Kodali R, Jahan R, Stephen MR, Yocum GT, Treven M, Poe MM, Li G, Yu OB, Hartzler BD, Zahn NM, Ernst M, Emala CW, Stafford DC, Cook JM, Arnold LA. Development of GABAA Receptor Subtype-Selective Imidazobenzodiazepines as Novel Asthma Treatments. Mol Pharm. 2016 Jun 6;13(6):2026-38. doi: 10.1021/acs.molpharmaceut.6b00159. Epub 2016 May 10. PubMed PMID: 27120014; PubMed Central PMCID: PMC4899155.
Teske KA, Bogart JW, Sanchez LM, Yu OB, Preston JV, Cook JM, Silvaggi NR, Bikle DD, Arnold LA. Synthesis and evaluation of vitamin D receptor-mediated activities of cholesterol and vitamin D metabolites. Eur J Med Chem. 2016 Feb 15;109:238-46. doi: 10.1016/j.ejmech.2016.01.002. Epub 2016 Jan 6. PubMed PMID: 26774929; PubMed Central PMCID: PMC4737989.
Teske KA, Yu O, Arnold LA. Inhibitors for the Vitamin D Receptor-Coregulator Interaction. Vitam Horm. 2016;100:45-82. doi: 10.1016/bs.vh.2015.10.002. Epub 2015 Nov 30. Review. PubMed PMID: 26827948; PubMed Central PMCID: PMC4740976.
2015
Kodali R., Guthrie ML, Poe MM, Stephen MR, Jahan R, Emala CW, Cook JM, Stafford DC, Arnold LA, “Metabolic Studies of Drug Candidates for Neurological Disorders and Asthma Based on GABA(A) Receptor Subtype Selective Ligands using Mass Spectrometry Shimadzu Journal 2015, 3(3), 64-68.
Clayton T, Poe MM, Rallapalli S, Biawat P, Savić MM, Rowlett JK, Gallos G, Emala CW, Kaczorowski CC, Stafford DC, Arnold LA, Cook JM. A Review of the Updated Pharmacophore for the Alpha 5 GABA(A) Benzodiazepine Receptor Model. Int J Med Chem. 2015;2015:430248. doi: 10.1155/2015/430248. Epub 2015 Nov 10. Review. PubMed PMID: 26682068; PubMed Central PMCID: PMC4657098.
Guthrie ML, Sidhu PS, Hill EK, Horan TC, Nandhikonda P, Teske KA, Yuan NY, Sidorko M, Rodali R, Cook JM, Han L, Silvaggi NR, Bikle DD, Moore RG, Singh RK, Arnold LA. Antitumor Activity of 3-Indolylmethanamines 31B and PS121912. Anticancer Res. 2015 Nov;35(11):6001-7. PubMed PMID: 26504023; PubMed Central PMCID: PMC4633305.
2014
Teske K, Nandhikonda P, Bogart JW, Feleke B, Sidhu P, Yuan N, Preston J, Goy R, Han L, Silvaggi NR, Singh RK, Bikle DD, Cook JM, Arnold LA. IDENTIFICATION OF VDR ANTAGONISTS AMONG NUCLEAR RECEPTOR LIGANDS USING VIRTUAL SCREENING. Nucl Receptor Res. 2014;1. doi: 10.11131/2014/101076. PubMed PMID: 25419525; PubMed Central PMCID: PMC4240308.
Teske K, Nandhikonda P, Bogart JW, Feleke B, Sidhu P, Yuan N, Preston J, Goy R, Arnold LA. Modulation of Transcription mediated by the Vitamin D Receptor and the Peroxisome Proliferator-Activated Receptor δ in the presence of GW0742 analogs. J Biomol Res Ther. 2014;3(1). doi: 10.4172/2167-7956.1000111. PubMed PMID: 25485183; PubMed Central PMCID: PMC4255951.
Sidhu PS, Teske K, Feleke B, Yuan NY, Guthrie ML, Fernstrum GB, Vyas ND, Han L, Preston J, Bogart JW, Silvaggi NR, Cook JM, Singh RK, Bikle DD, Arnold LA. Anticancer activity of VDR-coregulator inhibitor PS121912. Cancer Chemother Pharmacol. 2014 Oct;74(4):787-98. doi: 10.1007/s00280-014-2549-y. Epub 2014 Aug 9. PubMed PMID: 25107568; PubMed Central PMCID: PMC4177010.
McMurray KM, Distler MG, Sidhu PS, Cook JM, Arnold LA, Palmer AA, Plant LD. Glo1 inhibitors for neuropsychiatric and anti-epileptic drug development. Biochem Soc Trans. 2014 Apr;42(2):461-7. doi: 10.1042/BST20140027. Review. PubMed PMID: 24646261; PubMed Central PMCID: PMC4036232.
Sidhu PS, Nassif N, McCallum MM, Teske K, Feleke B, Yuan NY, Nandhikonda P, Cook JM, Singh RK, Bikle DD, Arnold LA. Development of novel Vitamin D Receptor-Coactivator Inhibitors. ACS Med Chem Lett. 2014 Feb 13;5(2):199-204. doi: 10.1021/ml400462j. PubMed PMID: 24799995; PubMed Central PMCID: PMC4007349.
McCallum MM, Pawlak AJ, Shadrick WR, Simeonov A, Jadhav A, Yasgar A, Maloney DJ, Arnold LA. A fluorescence-based high throughput assay for the determination of small molecule-human serum albumin protein binding. Anal Bioanal Chem. 2014 Mar;406(7):1867-75. doi: 10.1007/s00216-013-7560-3. Epub 2014 Jan 5. PubMed PMID: 24390461; PubMed Central PMCID: PMC3959589.
2013
Kawar N, Maclaughlan S, Horan TC, Uzun A, Lange TS, Kim KK, Hopson R, Singh AP, Sidhu PS, Glass KA, Shaw S, Padbury JF, Vorsa N, Arnold LA, Moore RG, Brard L, Singh RK. PT19c, Another Nonhypercalcemic Vitamin D2 Derivative, Demonstrates Antitumor Efficacy in Epithelial Ovarian and Endometrial Cancer Models. Genes Cancer. 2013 Nov;4(11-12):524-34. doi: 10.1177/1947601913507575. PubMed PMID: 24386512; PubMed Central PMCID: PMC3877664.
Nandhikonda P, Yasgar A, Baranowski AM, Sidhu PS, McCallum MM, Pawlak AJ, Teske K, Feleke B, Yuan NY, Kevin C, Bikle DD, Ayers SD, Webb P, Rai G, Simeonov A, Jadhav A, Maloney D, Arnold LA. Peroxisome proliferation-activated receptor δ agonist GW0742 interacts weakly with multiple nuclear receptors, including the vitamin D receptor. Biochemistry. 2013 Jun 18;52(24):4193-203. doi: 10.1021/bi400321p. Epub 2013 Jun 10. PubMed PMID: 23713684; PubMed Central PMCID: PMC3724348.
McCallum MM, Nandhikonda P, Temmer JJ, Eyermann C, Simeonov A, Jadhav A, Yasgar A, Maloney D, Arnold AL. High-throughput identification of promiscuous inhibitors from screening libraries with the use of a thiol-containing fluorescent probe. J Biomol Screen. 2013 Jul;18(6):705-13. doi: 10.1177/1087057113476090. Epub 2013 Feb 27. PubMed PMID: 23446699; PubMed Central PMCID: PMC3692575.
2012
Mukherjee S, Hanson AM, Shadrick WR, Ndjomou J, Sweeney NL, Hernandez JJ, Bartczak D, Li K, Frankowski KJ, Heck JA, Arnold LA, Schoenen FJ, Frick DN. Identification and analysis of hepatitis C virus NS3 helicase inhibitors using nucleic acid binding assays. Nucleic Acids Res. 2012 Sep 1;40(17):8607-21. doi: 10.1093/nar/gks623. Epub 2012 Jun 27. PubMed PMID: 22740655; PubMed Central PMCID: PMC3458564.
Nandhikonda P, Lynt WZ, McCallum MM, Ara T, Baranowski AM, Yuan NY, Pearson D, Bikle DD, Guy RK, Arnold LA. Discovery of the first irreversible small molecule inhibitors of the interaction between the vitamin D receptor and coactivators. J Med Chem. 2012 May 24;55(10):4640-51. doi: 10.1021/jm300460c. Epub 2012 May 16. PubMed PMID: 22563729; PubMed Central PMCID: PMC3364162.
Moore RG, Lange TS, Robinson K, Kim KK, Uzun A, Horan TC, Kawar N, Yano N, Chu SR, Mao Q, Brard L, DePaepe ME, Padbury JF, Arnold LA, Brodsky A, Shen TL, Singh RK. Efficacy of a non-hypercalcemic vitamin-D2 derived anti-cancer agent (MT19c) and inhibition of fatty acid synthesis in an ovarian cancer xenograft model. PLoS One. 2012;7(4):e34443. doi: 10.1371/journal.pone.0034443. Epub 2012 Apr 3. PubMed PMID: 22509304; PubMed Central PMCID: PMC3317945.
Chen Q, Yim PD, Yuan N, Johnson J, Cook JM, Smith S, Ionescu-Zanetti C, Wang ZJ, Arnold LA, Emala CW. Comparison of cell expression formats for the characterization of GABA(A) channels using a microfluidic patch clamp system. Assay Drug Dev Technol. 2012 Aug;10(4):325-35. doi: 10.1089/adt.2011.415. Epub 2012 May 10. PubMed PMID: 22574655; PubMed Central PMCID: PMC3419985.
2011
Féau C, Arnold LA, Kosinski A, Guy RK. Ligand competition binding assay for the androgen receptor. Methods Mol Biol. 2011;776:59-68. doi: 10.1007/978-1-61779-243-4_4. PubMed PMID: 21796520.
Atkinson JM, Shelat AA, Carcaboso AM, Kranenburg TA, Arnold LA, Boulos N, Wright K, Johnson RA, Poppleton H, Mohankumar KM, Féau C, Phoenix T, Gibson P, Zhu L, Tong Y, Eden C, Ellison DW, Priebe W, Koul D, Yung WK, Gajjar A, Stewart CF, Guy RK, Gilbertson RJ. An integrated in vitro and in vivo high-throughput screen identifies treatment leads for ependymoma. Cancer Cell. 2011 Sep 13;20(3):384-99. doi: 10.1016/j.ccr.2011.08.013. PubMed PMID: 21907928; PubMed Central PMCID: PMC3172881.
Sadana P, Hwang JY, Attia RR, Arnold LA, Neale G, Guy RK. Similarities and differences between two modes of antagonism of the thyroid hormone receptor. ACS Chem Biol. 2011 Oct 21;6(10):1096-106. doi: 10.1021/cb200092v. Epub 2011 Aug 15. PubMed PMID: 21815645; PubMed Central PMCID: PMC3199310.
Brard L, Lange TS, Robison K, Kim KK, Ara T, McCallum MM, Arnold LA, Moore RG, Singh RK. Evaluation of the first Ergocalciferol-derived, non hypercalcemic anti-cancer agent MT19c in ovarian cancer SKOV-3 cell lines. Gynecol Oncol. 2011 Nov;123(2):370-8. doi: 10.1016/j.ygyno.2011.07.002. Epub 2011 Jul 30. PubMed PMID: 21803404.
Johnson RL, Hwang JY, Arnold LA, Huang R, Wichterman J, Augustinaite I, Austin CP, Inglese J, Guy RK, Huang W. A quantitative high-throughput screen identifies novel inhibitors of the interaction of thyroid receptor beta with a peptide of steroid receptor coactivator 2. J Biomol Screen. 2011 Jul;16(6):618-27. doi: 10.1177/1087057111402199. Epub 2011 Apr 11. PubMed PMID: 21482722; PubMed Central PMCID: PMC3162318.
Hwang JY, Huang W, Arnold LA, Huang R, Attia RR, Connelly M, Wichterman J, Zhu F, Augustinaite I, Austin CP, Inglese J, Johnson RL, Guy RK. Methylsulfonylnitrobenzoates, a new class of irreversible inhibitors of the interaction of the thyroid hormone receptor and its obligate coactivators that functionally antagonizes thyroid hormone. J Biol Chem. 2011 Apr 8;286(14):11895-908. doi: 10.1074/jbc.M110.200436. Epub 2011 Feb 14. PubMed PMID: 21321127; PubMed Central PMCID: PMC3069392.
2010
Bikle DD, Teichert A, Arnold LA, Uchida Y, Elias PM, Oda Y. Differential regulation of epidermal function by VDR coactivators. J Steroid Biochem Mol Biol. 2010 Jul;121(1-2):308-13. doi: 10.1016/j.jsbmb.2010.03.027. Epub 2010 Mar 16. PubMed PMID: 20298785; PubMed Central PMCID: PMC2906691.
Reed D, Shen Y, Shelat AA, Arnold LA, Ferreira AM, Zhu F, Mills N, Smithson DC, Regni CA, Bashford D, Cicero SA, Schulman BA, Jochemsen AG, Guy RK, Dyer MA. Identification and characterization of the first small molecule inhibitor of MDMX. J Biol Chem. 2010 Apr 2;285(14):10786-96. doi: 10.1074/jbc.M109.056747. Epub 2010 Jan 15. PubMed PMID: 20080970; PubMed Central PMCID: PMC2856285.
2009
Féau C, Arnold LA, Kosinski A, Zhu F, Connelly M, Guy RK. Novel flufenamic acid analogues as inhibitors of androgen receptor mediated transcription. ACS Chem Biol. 2009 Oct 16;4(10):834-43. doi: 10.1021/cb900143a. PubMed PMID: 19645433; PubMed Central PMCID: PMC2763043.
Shahian T, Lee GM, Lazic A, Arnold LA, Velusamy P, Roels CM, Guy RK, Craik CS. Inhibition of a viral enzyme by a small-molecule dimer disruptor. Nat Chem Biol. 2009 Sep;5(9):640-6. doi: 10.1038/nchembio.192. Epub 2009 Jul 26. PubMed PMID: 19633659; PubMed Central PMCID: PMC2752665.
Hwang JY, Arnold LA, Zhu F, Kosinski A, Mangano TJ, Setola V, Roth BL, Guy RK. Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. J Med Chem. 2009 Jul 9;52(13):3892-901. doi: 10.1021/jm9002704. PubMed PMID: 19469546; PubMed Central PMCID: PMC2753520.
Teichert A, Arnold LA, Otieno S, Oda Y, Augustinaite I, Geistlinger TR, Kriwacki RW, Guy RK, Bikle DD. Quantification of the vitamin D receptor-coregulator interaction. Biochemistry. 2009 Feb 24;48(7):1454-61. doi: 10.1021/bi801874n. PubMed PMID: 19183053; PubMed Central PMCID: PMC2654718.
Féau C, Arnold LA, Kosinski A, Guy RK. A high-throughput ligand competition binding assay for the androgen receptor and other nuclear receptors. J Biomol Screen. 2009 Jan;14(1):43-8. doi: 10.1177/1087057108326662. PubMed PMID: 19171919; PubMed Central PMCID: PMC2632761.
2008
Arnold LA, Ranaivo P, Guy RK. Synthesis and characterization of BODIPY-labeled colchicine. Bioorg Med Chem Lett. 2008 Nov 15;18(22):5867-70. doi: 10.1016/j.bmcl.2008.07.068. Epub 2008 Jul 20. PubMed PMID: 18684625; PubMed Central PMCID: PMC2631555.
2007
Jouravel N, Sablin E, Arnold LA, Guy RK, Fletterick RJ. Interaction between the androgen receptor and a segment of its corepressor SHP. Acta Crystallogr D Biol Crystallogr. 2007 Nov;63(Pt 11):1198-200. doi: 10.1107/S0907444907045702. Epub 2007 Oct 17. PubMed PMID: 18007036; NIHMSID:NIHMS41534.
Arnold LA, Kosinski A, Estébanez-Perpiñá E, Fletterick RJ, Guy RK. Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. J Med Chem. 2007 Nov 1;50(22):5269-80. doi: 10.1021/jm070556y. Epub 2007 Oct 5. PubMed PMID: 17918822; PubMed Central PMCID: PMC2536611.
Estébanez-Perpiñá E, Arnold LA, Nguyen P, Rodrigues ED, Mar E, Bateman R, Pallai P, Shokat KM, Baxter JD, Guy RK, Webb P, Fletterick RJ. A surface on the androgen receptor that allosterically regulates coactivator binding. Proc Natl Acad Sci U S A. 2007 Oct 9;104(41):16074-9. doi: 10.1073/pnas.0708036104. Epub 2007 Oct 2. PubMed PMID: 17911242; PubMed Central PMCID: PMC1999396.
Estébanez-Perpiñá E, Arnold LA, Jouravel N, Togashi M, Blethrow J, Mar E, Nguyen P, Phillips KJ, Baxter JD, Webb P, Guy RK, Fletterick RJ. Structural insight into the mode of action of a direct inhibitor of coregulator binding to the thyroid hormone receptor. Mol Endocrinol. 2007 Dec;21(12):2919-28. doi: 10.1210/me.2007-0174. Epub 2007 Sep 6. PubMed PMID: 17823305; NIHMSID:NIHMS41531.
2006
Arnold LA, Kiplin Guy R. Synthesis of highly substituted dibenzo[b,f]azocines and their evaluation as protein kinase inhibitors. Bioorg Med Chem Lett. 2006 Oct 15;16(20):5360-3. doi: 10.1016/j.bmcl.2006.07.078. Epub 2006 Aug 4. PubMed PMID: 16890431.
Arnold LA, Estébanez-Perpiñá E, Togashi M, Shelat A, Ocasio CA, McReynolds AC, Nguyen P, Baxter JD, Fletterick RJ, Webb P, Guy RK. A high-throughput screening method to identify small molecule inhibitors of thyroid hormone receptor coactivator binding. Sci STKE. 2006 Jun 27;2006(341):pl3. doi: 10.1126/stke.3412006pl3. PubMed PMID: 16804159; NIHMSID:NIHMS41545.
2005
Arnold LA, Estébanez-Perpiñá E, Togashi M, Jouravel N, Shelat A, McReynolds AC, Mar E, Nguyen P, Baxter JD, Fletterick RJ, Webb P, Guy RK. Discovery of small molecule inhibitors of the interaction of the thyroid hormone receptor with transcriptional coregulators. J Biol Chem. 2005 Dec 30;280(52):43048-55. doi: 10.1074/jbc.M506693200. Epub 2005 Oct 31. PubMed PMID: 16263725; NIHMSID:NIHMS41544.
2004
Arnold LA, Luo W, Guy RK. Synthesis of medium ring heterocycles using an intramolecular Heck reaction. Org Lett. 2004 Aug 19;6(17):3005-7. doi: 10.1021/ol0487884. PubMed PMID: 15330669; NIHMSID:NIHMS41540.
Zijl AW, Arnold LA, Minnaard AJ, Feringa BL. Highly enantioselective copper-catalyzed allylic alkylation with phosphoramidite ligands. Advanced Synthesis & Catalysis. 2004 March; 346(4):413-420. doi: 10.1002/adsc.200303207.
2002
Feringa BL, Naasz R, Imbos R, Arnold LA. Copper-catalyzed Enantioselective Conjugate Addition Reactions of Organozinc Reagents. In: Krause N, editor. Modern Organocopper Chemistry Weinheim, Germany: Wiley-VCH Verlag GmbH; 2002. Chapter 7; p.224-258.
Arnold LA, Naasz R, Minnaard AJ, Feringa BL. Catalytic enantioselective synthesis of (-)-prostaglandin E1 methyl ester based on a tandem 1,4-addition-aldol reaction. J Org Chem. 2002 Oct 18;67(21):7244-54. doi: 10.1021/jo025987x. PubMed PMID: 12375950.
Bertozzi F, Pineschi M, Macchia F, Arnold LA, Minnaard AJ, Feringa BL. Copper phosphoramidite catalyzed enantioselective ring-opening of oxabicyclic alkenes: remarkable reversal of stereocontrol. Org Lett. 2002 Aug 8;4(16):2703-5. doi: 10.1021/ol026220u. PubMed PMID: 12153214.
2001
Mandoli A, Arnold LA, DeVries AH, Salvadori P, Feringa BL. New bidentate chiral phosphoramidites in copper catalyzed asymmetric 1,4-addition of diethylzinc to cyclic α,β-enones: Enantioselective tandem 1,4-addition-aldol reactions with 2-cyclopentenone. Tetrahedron, asymmetry. 2001 July; 12(13):1929-1937. doi: Doi 10.1016/S0957-4166(01)00348-2.
Arnold LA, Naasz R, Minnaard AJ, Feringa BL. Catalytic enantioselective synthesis of prostaglandin E(1) methyl ester using a tandem 1,4-addition-aldol reaction to a cyclopenten-3,5-dione monoacetal. J Am Chem Soc. 2001 Jun 20;123(24):5841-2. doi: 10.1021/ja015900+. PubMed PMID: 11403634.
Malda H, van Zijl AW, Arnold LA, Feringa BL. Enantioselective copper-catalyzed allylic alkylation with dialkylzincs using phosphoramidite ligands. Org Lett. 2001 Apr 19;3(8):1169-71. doi: 10.1021/ol0156289. PubMed PMID: 11348186.
Naasz R, Arnold LA, Minnaard AJ, Feringa BL. Highly Enantioselective Copper-Phosphoramidite Catalyzed Kinetic Resolution of Chiral 2-Cyclohexenones. Angew Chem Int Ed Engl. 2001 Mar 2;40(5):927-930. doi: 10.1002/1521-3773(20010302)40:5<927::AID-ANIE927>3.0.CO;2-K. PubMed PMID: 29712175.
Naasz R, Arnold LA, Minnaard AJ, Feringa BL. Enantioselective synthesis of bicyclic compounds via catalytic 1,4-addition-ring closing metathesis. Chemical communications (Cambridge, England). 2001; (8):735-736. doi: Doi 10.1039/B100283j.
2000
Arnold LA, Imbos R, Mandoli A, deVries AH, Naasz R, Feringa BL. Enantioselective catalytic conjugate addition of dialkylzinc reagents using copper-phosphoramidite complexes; Ligand variation and non-linear effects. Tetrahedron. 2000 April; 56(18):2865-2878. doi: Doi 10.1016/S0040-4020(00)00142-3.
Bertozzi F, Crotti P, Macchia F, Pineschi M, Arnold A, Feringa BL. A new catalytic and enantioselective desymmetrization of symmetrical methylidene cycloalkene oxides. Org Lett. 2000 Apr 6;2(7):933-6. doi: 10.1021/ol005584o. PubMed PMID: 10768190.
1999
Bertozzi F, Crotti P, Pineschi M, Arnold LA, Feringa BL. A new diastereo- and enantioselective copper-catalyzed conversion of alkynyl epoxides into alpha-allenic alcohols. Tetrahedron letters. 1999 June; 40(26):4893-4896. doi: Doi 10.1016/S0040-4039(99)00905-3.
Naasz R, Arnold LA, Pineschi M, Keller E, Feringa BL. Catalytic enantioselective annulations via 1,4-addition-aldol cyclization of functionalized organozinc reagents. Journal of the American Chemical Society. 1999 February; 121(5):1104-1105. doi: Doi 10.1021/Ja983693g.
1998
Baldalassi F, Crotti P, Macchia F, Pinetischi M, Arnold LA, Feringa BL. Catalytic enantioselective carbon-carbon bond formation by addition of dialkylzinc reagents to cyclic 1,3-diene monoepoxides. Tetrahedron letters. 1998 October; 39(42):7795-7798. doi: Doi 10.1016/S0040-4039(98)01704-3.
1997
Feringa BL, Pineschi M, Arnold LA, Imbos R, deVries AH. Highly enantioselective catalytic conjugate addition and tandem conjugate addition-aldol reactions of organozinc reagents. Angewandte Chemie (International ed. in English). 1997 December; 36(23):2620-2063. doi: DOI 10.1002/anie.199726201.