Lennart Bunch
Professor
Medicinal Chemistry
Jagtvej 162
2100 København Ø
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β-Indolyloxy Functionalized Aspartate Analogs as Inhibitors of the Excitatory Amino Acid Transporters (EAATs)
Liu, N., Jensen, Anders A. & Bunch, Lennart, 2020, In: ACS Medicinal Chemistry Letters. 11, 11, p. 2212-2220 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Unprecedented migration of N-alkoxycarbonyl groups in protected pyroglutaminol
Bunch, Lennart, Norrby, P., Frydenvang, Karla Andrea, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2001, In: Organic Letters. 3, 3, p. 433-5 3 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Transition Metal-Free Synthesis of meta-Bromo- and meta-Trifluoromethylanilines from Cyclopentanones by a Cascade Reaction
Staudt, Markus, Cetin, A. & Bunch, Lennart, 2022, In: Chemistry: A European Journal. 28, 10, 5 p., 202102998.Research output: Contribution to journal › Journal article › Research › peer-review
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The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells
Cuesta, E. P., Christensen, S., Jensen, Anders A., Jensen, N. F., Bunch, Lennart, Rømer, M. U. K., Brünner, N., Stenvang, Jan & Pedersen, Stine Helene Falsig, 2015, In: B M C Cancer. 15, 1, 17 p., 411.Research output: Contribution to journal › Journal article › Research › peer-review
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The Screening and Design of Allosteric Kinase Inhibitors
Wu, P., Dinér, P. & Bunch, Lennart, 2019, Kinase Drug Discovery: Modern Approaches. 1. ed. Royal Society of Chemistry, p. 34-60Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Research › peer-review
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Tetrabutylammonium Fluoride (TBAF) as a Mild and Versatile Reagent for Cleaving Boroxazolidones to their Corresponding Free α-Amino Acids
Poulie, Christian Bernard Matthijs & Bunch, Lennart, Mar 2017, In: European Journal of Organic Chemistry. 11, p. 1475-1478Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis of phenol derivatives from cyclopentenones with arynes as key intermediates
Telese, D., Staudt, Markus & Bunch, Lennart, 2022, In: Results in Chemistry. 4, 7 p., 100412.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis of Polysubstituted Meta-Halophenols by Anion-Accelerated 2π-Electrocyclic Ring-Opening
Staudt, Markus, Sølling, Theis Ivan & Bunch, Lennart, 2021, In: Chemistry - A European Journal. 27, 42, p. 10941–10947 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis of (3-hydroxy-pyrazolin-5-yl)glycine based ligands interacting with ionotropic glutamate receptors
Pinto, A., Tamborini, L., Mastronardi, F., Ettari, R., Safoz, Y., Bunch, Lennart, Nielsen, Birgitte, Jensen, Anders A., De Micheli, C. & Conti, P., 2014, In: European Journal of Medicinal Chemistry. 75, p. 151-158 8 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and receptor binding affinity of new selective GluR5 ligands
Bunch, Lennart, Johansen, T. H., Bräuner, Hans, Stensbøl, T. B., Johansen, Tommy Nørskov, Krogsgaard-Larsen, Povl & Madsen, Ulf, Apr 2001, In: Bioorganic & Medicinal Chemistry. 9, 4, p. 875-9Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and pharmacological characterization of conformationally restricted 2-amino-Adipic acid analogs and carboxycyclopropyl glycines as selective metabotropic glutamate 2 receptor agonists
Staudt, Markus, Liu, N., Malhaire, F., Doroudian, Yasaman, Prézeau, L., Renard, E., Hasanpour, Z., Pin, J. P. & Bunch, Lennart, 2024, In: European Journal of Medicinal Chemistry. 266, 11 p., 116157.Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis and Selective Functionalization of [1,2,4]Triazolo[4,3-a]pyrazines
Demmer, C. S., Jorgensen, M., Kehler, J., Bunch, Lennart & Rasmussen, L. K., 2015, In: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 26, 4, p. 519-524 6 p.Research output: Contribution to journal › Letter › Research › peer-review
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Synthesis and Pharmacological Characterization of the Selective GluK1 Radioligand (S)-2-Amino-3-(6-[3H]-2,4-dioxo-3,4-dihydrothieno[3,2-d]pyrimidin-1(2H)-yl)propanoic acid ([3H]-NF608)
Alcaide, A., Marconi, L., Marek, A., Haym, I., Nielsen, Birgitte, Møllerud, S., Jensen, M., Conti, P., Pickering, Darryl S & Bunch, Lennart, 2016, In: MedChemComm. 7, p. 2136-2144 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Subtype selective kainic acid receptor agonists: discovery and approaches to rational design
Bunch, Lennart & Krogsgaard-Larsen, Povl, 2009, In: Medicinal Research Reviews. 29, 1, p. 3-28Research output: Contribution to journal › Review › Research › peer-review
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Study of Oxidative Cyclization Using PhI(OAc)(2) in the Formation of Benzo[4,5]thiazolo[2,3-c][1,2,4]triazoles and Related Heterocycles - Scope and Limitations
Demmer, C. S., Jorgensen, M., Kehler, J. & Bunch, Lennart, Jun 2014, In: SYNLETT: Accounts and Rapid Communications in Chemical Synthesis. 25, 9, p. 1279-1282 4 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity-relationship study of N-acyl-N-phenylpiperazines as potential inhibitors of the excitatory amino acid transporters (EAATs): Improving the potency of a micromolar screening hit is not truism
Huynh, Tri Hien Viet, Demmer, C. S., Abrahamsen, B., Marcher, Emil, Frykman, M., Jensen, Anders A. & Bunch, Lennart, 2013, In: SpringerPlus. 2, p. 112Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity relationship study of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitor 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101) and absolute configurational assignment using infrared and vibrational circular dichroism spectroscopy in combination with ab initio hartree-fock calculations
Huynh, Tri Hien Viet, Shim, I., Bohr, H., Abrahamsen, B., Nielsen, Birgitte, Jensen, Anders A. & Bunch, Lennart, 2012, In: Journal of Medicinal Chemistry. 55, 11, p. 5403-12 10 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-activity relationship study of first selective inhibitor of excitatory amino acid transporter subtype 1: 2-amino-4-(4-methoxyphenyl)-7-(naphthalen-1-yl)-5-oxo-5,6,7,8-tetrahydro-4H-chromene-3-carbonitrile (UCPH-101)
Erichsen, M. N., Huynh, Tri Hien Viet, Abrahamsen, B., Bastlund, J. F., Bundgaard, C., Monrad, O., Bekker-Jensen, A., Nielsen, C. W., Frydenvang, Karla Andrea, Jensen, Anders A. & Bunch, Lennart, 2010, In: Journal of Medicinal Chemistry. 53, 19, p. 7180–7191Research output: Contribution to journal › Journal article › Research › peer-review
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Structure-Activity Relationship Study of Ionotropic Glutamate Receptor Antagonist (2S,3R)-3-(3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid
Krogsgaard-Larsen, N., Storgaard, M., Møller, C., Demmer, C. S., Hansen, J., Han, L., Monrad, R. N., Nielsen, Birgitte, Tapken, D., Pickering, Darryl S, Kastrup, Jette Sandholm Jensen, Frydenvang, Karla Andrea & Bunch, Lennart, 2015, In: Journal of Medicinal Chemistry. 58, 15, p. 6131-50 20 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Stereoselective chemoenzymatic synthesis of the four stereoisomers of l-2-(2-carboxycyclobutyl)glycine and pharmacological characterization at human excitatory amino acid transporter subtypes 1, 2, and 3
Faure, S., Jensen, Anders A., Maurat, V., Gu, X., Sagot, E., Aitken, D. J., Bolte, J., Gefflaut, T. & Bunch, Lennart, 2006, In: Journal of Medicinal Chemistry. 49, 22, p. 6532-8 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp3)-H Activation Strategy and Structure-Activity Relationship Studies at the Ionotropic Glutamate Receptors
Kayser, S., Hansen, J. C., Staudt, Markus, Moroz, A., Larsen, Y., Temperini, Piero, Yi, F., Syrenne, J. T., Krogsgaard-Larsen, N., Iliadis, S., Nielsen, Birgitte, Hansen, K. B., Pickering, Darryl S & Bunch, Lennart, 2020, In: ACS Chemical Neuroscience. 11, p. 674-701 28 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Stereocontrolled synthesis and pharmacological evaluation of azetidine-2,3-dicarboxylic acids at NMDA receptors
Sivaprakasam, M., Hansen, K. B., David, O., Nielsen, Birgitte, Traynelis, S. F., Clausen, Rasmus Prætorius, Couty, F. & Bunch, Lennart, 2009, In: ChemMedChem. 4, 1, p. 110-117Research output: Contribution to journal › Journal article › Research › peer-review
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Semi-synthesis of novel buprenorphine derivatives and their anti-nociceptive properties and dependency potential
Hasanpour, Z., Salehi, P., Bunch, Lennart, Khoramjouy, M., Bararjanian, M., Stærk, Dan & Faizi, M., 2021, In: Canadian Journal of Chemistry. 99, 11, p. 910-919Research output: Contribution to journal › Journal article › Research › peer-review
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Revisiting the Quinoxalinedione scaffold in the Construction of New Ligands for the Ionotropic Glutamate Receptors.
Demmer, C. S., Rombach, D., Liu, N., Nielsen, Birgitte, Pickering, Darryl S & Bunch, Lennart, 1 Dec 2017, In: A C S Chemical Neuroscience. 8, 11, p. 2477-2495 19 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Review on modern advances of chemical methods for the introduction of a phosphonic acid group
Demmer, C. S., Krogsgaard-Larsen, N. & Bunch, Lennart, 2011, In: Chemical Reviews. 111, 12, p. 7981-8006Research output: Contribution to journal › Review › Research › peer-review
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Regioselective lithiation and functionalization of 3-(benzyloxy)isothiazole: Application to the synthesis of thioibotenic acid
Bunch, Lennart, Krogsgaard-Larsen, Povl & Madsen, Ulf, 5 Apr 2002, In: Journal of Organic Chemistry. 67, 7, p. 2375-2377Research output: Contribution to journal › Journal article › Research › peer-review
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Rational design, synthesis, and pharmacological evaluation of 2-azanorbornane-3-exo,5-endo-dicarboxylic acid: a novel conformationally restricted glutamic acid analogue
Bunch, Lennart, Liljefors, T., Greenwood, J. R., Frydenvang, Karla Andrea, Bräuner, Hans, Krogsgaard-Larsen, Povl & Madsen, Ulf, 2003, In: Journal of Organic Chemistry. 68, 4, p. 1489-95 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Rational design and enantioselective synthesis of (1R,4S,5R,6S)-3-azabicyclo[3.3.0]octane-4,6-dicarboxylic acid - a novel inhibitor at human glutamate transporter subtypes 1, 2, and 3
Bunch, Lennart, Nielsen, Birgitte, Jensen, Anders A. & Bräuner, Hans, 2006, In: Journal of Medicinal Chemistry. 49, 1, p. 172-8 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Rational Design, Synthesis and Pharmacological Evaluation of the (2R)- and (2S)-Stereoisomers of 3-(2-Carboxypyrrolidinyl)-2-methyl Acetic Acid as Ligands for the Ionotropic Glutamate Receptors.
Rasmussen, J., Storgaard, M., Pickering, Darryl S & Bunch, Lennart, 7 Mar 2011, In: ChemMedChem. 6, 3, p. 498-504 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Profiling substrate specificity of two series of phenethylamine analogs at monoamine oxidase A and B
Heuson, E., Storgaard, M., Huynh, Tri Hien Viet, Charmantray, F., Gefflaut, T. & Bunch, Lennart, 2014, In: Organic & Biomolecular Chemistry. 12, 43, p. 8689-8695 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Probing for improved potency and in vivo bioavailability of excitatory amino acid transporter subtype 1 inhibitors UCPH-101 and UCPH-102: Design, synthesis and pharmacological evaluation of substituted 7-biphenyl analogs
Erichsen, M. N., Hansen, J., Artacho Ruiz, J., Demmer, C. S., Abrahamsen, B., Bastlund, J. F., Bundgaard, C., Jensen, Anders A. & Bunch, Lennart, 2014, In: Neurochemical Research. 39, 10, p. 1964-1979 16 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Physiology, pharmacology and pathophysiology of the pH regulatory transport proteins NHE1 and NBCn1: similarities, differences, and implications for cancer therapy
Bødtkjer, E., Bunch, Lennart & Pedersen, Stine Helene Falsig, 2012, In: Current Pharmaceutical Design. 18, 10, p. 1345-1371 27 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Pharmacological characterization of (4R)-alkyl glutamate analogues at the ionotropic glutamate receptors: focus on subtypes iGlu5-7
Bunch, Lennart, Gefflaut, T., Alaux, S., Sagot, E., Nielsen, Birgitte & Pickering, Darryl S, 2009, In: European Journal of Pharmacology. 609, p. 1-4Research output: Contribution to journal › Journal article › Research › peer-review
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Pharmacological and structural characterization of conformationally restricted (S)-glutamate analogues at ionotropic glutamate receptors
Juknaite, L., Venskutonyte, R., Assaf, Z., Faure, S., Gefflaut, T., Aitken, D. J., Nielsen, Birgitte, Gajhede, Michael, Kastrup, Jette Sandholm Jensen, Bunch, Lennart, Frydenvang, Karla Andrea & Pickering, Darryl S, 2012, In: Journal of Structural Biology. 180, 1, p. 39-46Research output: Contribution to journal › Journal article › Research › peer-review
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New insights into the structure-activity-relationship of selective excitatory amino acid transporter subtype 1 (EAAT1) inhibitors UCPH-101 and UCPH-102
Hansen, S. W., Erichsen, M. N., Huynh, Tri Hien Viet, Ruiz, J. A., Haym, I., Bjørn-Yoshimoto, Walden, Abrahamsen, B., Hansen, Jeanette Venla, Storgaard, M., Eriksen, A. L., Jensen, Anders A. & Bunch, Lennart, 2016, In: ChemMedChem. 11, 4, p. 382-402 21 p.Research output: Contribution to journal › Journal article › Research › peer-review
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New Palladium-Catalyzed Domino Reaction with Intramolecular Ring Closure of an N-(2-Chloro-3-heteroaryl) arylamide: First Synthesis of Oxazolo[4,5-b] pyrazines
Demmer, C. S., Hansen, J. C., Kehler, J. & Bunch, Lennart, 24 Mar 2014, In: Advanced Synthesis & Catalysis. 356, 5, p. 1047-1055 9 p.Research output: Contribution to journal › Journal article › Research › peer-review
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New 4-Functionalized Glutamate Analogues Are Selective Agonists at Metabotropic Glutamate Receptor Subtype 2 or Selective Agonists at Metabotropic Glutamate Receptor Group III
Huynh, Tri Hien Viet, Erichsen, M. N., Tora, A. S., Goudet, C., Sagot, E., Assaf, Z., Thomsen, C., Brodbeck, R., Stensbol, T. B., Bjørn-Yoshimoto, Walden, Nielsen, Birgitte, Pin, J., Gefflaut, T. & Bunch, Lennart, 2016, In: Journal of Medicinal Chemistry. 59, 3, p. 914-924 11 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Molecular recognition of two 2,4-syn-functionalized (S)-glutamate analogues by the kainate receptor GluK3 ligand-binding domain
Venskutonyte, R., Larsen, A. P., Frydenvang, Karla Andrea, Gajhede, Michael, Gefflaut, T., Pickering, Darryl S, Bunch, Lennart & Kastrup, Jette Sandholm Jensen, 2014, In: ChemMedChem. 9, 10, p. 2254-2259 6 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Mixed cyano-gilman cuprates - Advances in conjugate addition to alpha,beta-unsaturated pyroglutaminol
Bunch, Lennart, Krogsgaard-Larsen, Povl & Madsen, Ulf, Jan 2002, In: Synthesis. 1, p. 31-33Research output: Contribution to journal › Journal article › Research › peer-review
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Medicinal chemistry of competitive kainate receptor antagonists
Larsen, A. M. & Bunch, Lennart, 16 Feb 2011, In: ACS Chemical Neuroscience. 2, 2, p. 60-74Research output: Contribution to journal › Review › Research › peer-review
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Introduction to drug design and discovery
Krogsgaard-Larsen, Povl & Bunch, Lennart, 2010, Textbook of drug design and discovery. Krogsgaard-Larsen, P., Strømgaard, K. & Madsen, U. (eds.). 4 ed. Boca Raton: CRC Press, p. 1-13Research output: Chapter in Book/Report/Conference proceeding › Book chapter › Education
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In vitro ADME characterization of a very potent 3-acylamino-2-aminopropionic acid-derived GluN2C-NMDA receptor agonist and its ester prodrugs
Bechthold, E., Grey, L., Diamant, E., Schmidt, J., Steigerwald, R., Zhao, F., Hansen, K. B., Bunch, Lennart, Clausen, Rasmus Prætorius & Wünsch, B., 2023, In: Biological Chemistry. 404, 4, p. 255-265Research output: Contribution to journal › Journal article › Research › peer-review
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Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity-Relationship Study
Hansen, S. W., Erichsen, M. N., Fu, B., Bjørn-Yoshimoto, Walden, Abrahamsen, B., Hansen, J. C., Jensen, Anders A. & Bunch, Lennart, 2016, In: Journal of Medicinal Chemistry. 59, 19, p. 8757-8770 14 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Identification and Structure-Activity Relationship Study of Imidazo[1,2-a]pyridine-3-amines as First Selective Inhibitors of Excitatory Amino Acid Transporter Subtype 3 (EAAT3)
Wu, P., Bjørn-Yoshimoto, Walden, Staudt, Markus, Jensen, Anders A. & Bunch, Lennart, 2019, In: ACS Chemical Neuroscience. 10, p. 4414-4429Research output: Contribution to journal › Journal article › Research › peer-review
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Ibotenic acid and thioibotenic acid: a remarkable difference in activity at group III metabotropic glutamate receptors
Hermit, M. B., Greenwood, J. R., Nielsen, Birgitte, Bunch, Lennart, Jørgensen, Charlotte Grube, Vestergaard, H. T., Stensbøl, T. B., Sanchez, C., Krogsgaard-Larsen, Povl, Madsen, Ulf & Bräuner, Hans, 23 Feb 2004, In: European Journal of Pharmacology. 486, 3, p. 241-50Research output: Contribution to journal › Journal article › Research › peer-review
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Heterocycles as nonclassical bioisosteres of alpha-amino acids
Poulie, Christian Bernard Matthijs & Bunch, Lennart, Feb 2013, In: ChemMedChem. 8, 2, p. 205-215Research output: Contribution to journal › Journal article › Research › peer-review
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Gram-scale solution-phase synthesis of selective sodium bicarbonate Co-transport Inhibitor S0859: in vitro efficacy studies in breast cancer cells
Larsen, A. M., Krogsgaard-Larsen, N., Lauritzen, G., Olesen, C. W., Hansen, S. H., Bødtkjer, E., Pedersen, Stine Helene Falsig & Bunch, Lennart, 2012, In: ChemMedChem. 7, 10, p. 1808-1814 7 p.Research output: Contribution to journal › Journal article › Research › peer-review
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Glutamate receptor agonists: stereochemical aspects
Vogensen, S. B., Greenwood, J. R., Bunch, Lennart & Clausen, Rasmus Prætorius, Apr 2011, In: Current Topics in Medicinal Chemistry. 11, 7, p. 887-906Research output: Contribution to journal › Review › Research › peer-review
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Functionalization of Oxazolo[4,5-b]pyrazines by Deprotometallation
Bisballe, N., Hedidi, M., Demmer, C. S., Chevallier, F., Roisnel, T., Dorcet, V., Halauko, Y. S., Ivashkevich, O. A., Matulis, V. E., Bentabed-Ababsa, G., Bunch, Lennart & Mongin, F., 7 Aug 2018, In: European Journal of Organic Chemistry. 29, p. 3904-3913Research output: Contribution to journal › Journal article › Research › peer-review
ID: 1302517
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329
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The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells
Research output: Contribution to journal › Journal article › Research › peer-review
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195
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Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors
Research output: Contribution to journal › Journal article › Research › peer-review
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Synthesis of phenol derivatives from cyclopentenones with arynes as key intermediates
Research output: Contribution to journal › Journal article › Research › peer-review
Published