Publikationen & Patente

2018

  1. Bhatia, S.; Krieger. V.; Groll, M.; Osko, J. D.; Reßing, N., Borkhardt, A., Kurz, T.; Christianson, D. W.; Hauer, J. (co-senior author); Hansen, F. K.
    "Discovery of the first-in-class dual histone deacetylase-proteasome inhibitor"
    J. Med. Chem.     2018, DOI: 10.1021/acs.jmedchem.8b01487
  2. Reßing, N.; Marquardt, V.; Gertzen, C. G. W.; Schöler, A.; Schramm, A.; Kurz, T.; Aigner, A.; Remke, M.; Hansen, F. K.
    "Design, synthesis and biological evaluation of β-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity"
    MedChemComm     2018, DOI: 10.1039/C8MD00454D.
  3. Diedrich, D.; Stenzel, K.; Hesping, E.; Antonova-Koch, Y.; Gebru, T.; Duffy, S.; Fisher, G.; Schöler, A.; Meister, S.; Kurz, T.; Avery, V. M.; Winzeler, E. A.; Held, J.; Andrews, K. T.* (co-senior author), Hansen, F. K.*
    "One-pot, multi-component synthesis and structure-activity relationships of peptoid-based histone deacetylase (HDAC) inhibitors targeting malaria Parasites"                                                       
    Eur. J. Med. Chem.     2018, 158, 801-813.
  4. Porter, N. J.; Osko, J. D.; Diedrich, D.; Kurz, T.; Hooker, J. M.; Hansen, F. K.; Christianson, D. W. "HDAC6-Selective Phynylhydroxamate Inhibitors and the Influence of Capping Groups on Hydroxamate-Zinc Denticity"                                                                                                        J. Med. Chem. 2018, 61, 8054-8060.
  5. Mackwitz, M. K. W.; Hamacher, A.; Osko, J. D.; Held, J.; Schöler, A.; Christianson, D. W.; Kassack, M. U;. Hansen, F. K.
    “Multicomponent synthesis and binding mode of imidazo[1,2-a]pyridine-capped selective HDAC6 inhibitors”
    Org. Lett. 2018, 20, 3255-3258.
  6. Bhatia, S.; Diedrich, D.; Frieg, B.; Ahlert, H.; Stein, St.; Bopp, B.; Lang, F.; Zang, T.; Kroeger, T.; Ernst, Th.; Koegler, G.; Krieg, A.; Luedeke, St.; Kunkel, H.; Rodrigues Moita, A. J.; Kassack, M. U.; Marquardt, V.; Opitz, F.; Oldenburg, M.; Remke, M.; Babor, F.; Grez, M.; Hochhaus, A.; Borkhardt, A.; Groth, G.; Nagel-Steger, L.; Jose, J.; Kurz, Th.; Gohlke, H.; Hansen, F. K.* (co-senior author), Hauer, J.* 
    “Targeting HSP90 dimerization via the C-terminus is effective in imatinib resistant CML and lacks heat shock response” 
    Blood 2018, 132, 307-320.

 

 

2017

  1. Stenzel, K.; Chua, M. J.; Duffy, S.; Antonova-Koch, Y.; Meister, S.; Hamacher, A.; Kassack, M. U.; Winzeler, E. A.; Avery, V. M.; Kurz, T.; Andrews, K. T.* (co-senior author); Hansen, F. K.*
    Design and synthesis of terephthalic acid-based histone deacetylase inhibitors with dual stage anti-Plasmodium activity
    ChemMedChem 2017, 12, 1627-1636.
  2. Stenzel, K.; Hamacher, A.; Hansen, F. K.; Gertzen, C. G. W.; Senger, J.; Marquardt, V.; Marek, L.; Marek, M.; Romier, C.; Remke, M.; Jung, M.; Gohlke, H.; Kassack, M. U.; Kurz; T.
    Alkoxyurea-based Histone Deacetylase Inhibitors Increase Cisplatin Chemosensitivity
    J. Med. Chem. 2017, 60, 5334-5348.
  3. Krieger, V.; Hamacher,  A.; Gertzen,  C. G. W.; Senger, J.; Zwinderman, M. R. H.; Marek, M.; Romier, C.; Dekker, F. J.; Kurz, T.; Jung, M.; Gohlke, H.; Kassack, M. U.; Hansen, F. K.
    Design, multicomponent synthesis and anticancer activity of a focused histone deacetylase (HDAC) inhibitor library with peptoid-based cap groups
    J. Med. Chem. 2017, 60, 5493-5506.
  4. Stenzel, K.; Chakrabarti, A.; Melesina, J.; Hansen, F. K.; Lancelot, J.; Herkenhöhner, S.; Lungerich, B.; Marek, M.; Romier, C.; Pierce, R. J.; Sippl, W.; Jung, M.; Kurz, T.
    Isophthalic acid-based HDAC Inhibitors as Potent Inhibitors of HDAC8 from Schistosoma mansoni
    Arch. Pharm. Chem. Life Sci. 2017, 350, e1700096.
  5. Avelar, L. A.; Held, J.; Engel, J. A.; Sureechatchaiyan, P.; Hansen, F. K.; Hamacher, A.; Kassack, M. U.; Mordmüller, B.; Andrews, K. T.; Kurz, T.
    Design and Synthesis of Novel Anti-Plasmodial Histone Deacetylase Inhibitors Containing an Alkoxyamide Connecting Unit
    Arch. Pharm. Chem. Life Sci. 2017, 350, e1600347.
  6. Krieger, V.; Ciglia, E.; Thoma, R.; Vasylyeva, V.; Frieg, B.; de Sousa Amadeu, N.; Kurz, T.; Janiak, C.; Gohlke, H.; Hansen, F. K.
    α-Aminoxy Peptoids: A Unique Peptoid Backbone with a Preference for Cis-Amide Bonds
    Chem. Eur. J.     2017, 23, 3699–3707.

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2014

  1. Burda, E.; Rademann, J.
    Catalytic activation of pre-substrates via dynamic fragment assembly on protein templates.
    Nature Comm. 2014, 5, 517.
  2. Preidl, J. J.; Gnanaprassam, V.S.; Lisurek, M.; Saupe, J.; Horstkorte, R.; Rademann, J.
    Fluorescent Mimetics of CMP-Neu5Ac are Highly Potent and Cell-Permeable Polarization Probes of Eukaryotic and Bacterial Sialyltransferases and Inhibit Cellular Sialylation.
    Angew. Chem. Int. Ed. 2014, 53, 5700; Angew. Chem. 2014, 126, 5808.
  3. Schwan, G.; Barbar Asskar, G.; Höfgen, N.; Kubicova, L.; Funke, U.; Egerland, U.; Zahn, M.; Nieber, K.; Scheunemann, M.; Sträter, N.; Brust, P.; Briel, D.
    Fluorine-containing 6,7-dialkoxybiaryl-based inhibitors for phosphodiesterase 10A: Synthesis and in vitro evaluation of inhibitory potency, selectivity, and metabolism.
    ChemMedChem 2014, 9, 1476.

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2013

  1. Fernández-Bachiller, M. I.; Lisurek, M.; Horatscheck, A.; Rademann, J.
    Alzheimer´s disease: Identification and development of BACE-1 binding fragments and inhibitors by Dynamic Ligation Screening (DLS).
    ChemMedChem 2013, 8, 1041.
  2. Arkona, C.; Rademann, J. Propargyl
    Amides as Irreversible Inhibitors of Cysteine Proteases -- A Lesson on the Biological Reactivity of Alkynes.
    Angew. Chem. 2013, 125, 8368; Angew. Chem. Int. Ed. 2013, 52, 8210.
  3. Koschek, K.; Dathe, M.; Rademann, J.
    Effects of Charge and Charge Distribution on the Cellular Uptake of Multivalent Arginine-Containing Peptide-Polymer Conjugates.
    ChemBioChem 2013, 14, 1982-1990.
  4. Schäfer, G.; Milic, J.; Eldahshan, A.; Götz, F.; Zühlke, K.; Schillinger, C.; Kreuchwig, A.; Elkins, J. M.; Azeez, K. R. A.; Oder, A.; Moutty, M. C.; Masada, N.; Beerbaum, M.; Schlegel, B. ; Niquet, S.; Schmieder, P.; Krause, G.; v. Kries, J. P.; Cooper, D. M. F.; Knapp, S.; Rademann, J.; Rosenthal, W.; Klussmann, E.
    Highly Functionalized Terpyridines as Competitive Inhibitors of AKAP-PKA Interactions.
    Angew. Chem. 2013, 125, 12409; Angew. Chem. Int. Ed. 2013, 52, 12187.

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2012

  1. Funke, U.; Deuther-Conrad, W.; Schwan, G.; Maisonial, A.; Scheunemann, M.; Fischer, S.; Hiller, A.; Briel, D.; Brust, P.
    Radiosynthesis and radiotracer properties of a 7-(2-[18F]fluoroethoxy)-6-methoxy-pyrrolidinylquinazoline for imaging of phosphodiesterase 10A with PET.
    Pharmaceuticals 2012, 5, 169.

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2010

  1. Briel, D.; Rudolph, I.; Unverferth, K.
    Synthesis of disubstituted 1,4-diazepines as potential benzodiazepine agonists.
    Pharmazie 2010, 65, 641.
  2. Briel, D.; Rybak, A.; Kronbach, C.; Unverferth, K.; Gonzales Tannarro C. M.; Gütschow, M.
    Thieno[2,3-d]pyrimidines and -[1,3]Oxazines as Glutamate Antagonists and Investigations on the Potency towards Human Leukocyte Elastase.
    J. Heterocycl. Chem. 2010, 47, 634.
  3. Briel, D.; Rybak, A.; Kronbach, C.; Unverferth. K.
    Substituted 2-Aminothiophen-derivatives: A potential new class of GluR6-Antagonists.
    Eur. J. Med. Chem. 2010, 45, 69.

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2009

  1. Briel, D.; Askar, G.B; Ortwein, J.; Unverferth, K.
    A convenient synthesis of furans using bromacetylpyran-2-one.
    Pharmazie 2009, 64, 477.
  2. Briel, D.; Rybak, A.; Mann, S.; Kronbach, C.; Unverferth, K.
    Synthesis of Thieno[2,3-d]oxazines and Thieno[2,3-d]thiazines as Subtype Specific Kainate Receptor Antagonists.
    Curr. Med. Chem. 2009, 16, 4704.

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2008

  1. Rybak, A.; Kronbach, C.; Unverferth, K.; Briel, D.
    Thieno[2,3-d]pyrimidines as Abtagonists of the Glutamate Receptors.
    Pharmazie 2008, 63, 823.

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2007

  1. Drescher, S.; Ramsbeck, D.; Briel, D. Dobner, B.
    Selective Nucleophilic Substitution Reactions in 2,4,6-Trisulfanylsubstituted Pyrimidin-5-carbonitriles by Secondary Amines.
    J. Heterocyclic Chem.     2007, 44, 757.

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2005

  1. Briel, D.; Drescher, S.; Dobner, B.
    Selective Nucleophilic Replacement of the Benzylsulfanyl Group in 2,4-Disulfanyl-substituted Thieno[2,3-d]pyrimidin-6-carboxylic Acid Derivatives by Sec. Amines.
    J. Heterocyclic Chem. 2005, 42, 841.
  2. Briel, D.; Aurich, R.; Egerland, U.; Unverferth, K.
    Synthesis of Substituted 6‑Phenylpyrazolo[3,4‑d]pyrimidines with Potential Adenosin-A2A Antagonistic Activity.
    Pharmazie 2005, 60, 732.
  3. Briel, D.
    Synthesis and Conversion of 3-(2-Hydroxythiobenzamido)benzo[b]furans.
    Heterocycles 2005, 65, 1295.
  4. Briel, D.
    Synthesis of Thieno[2,3-d]pyrimidines from 6-Imino-6H-1,3-thiazine Hydroperchlorates.
    Pharmazie 2005, 60, 75.
  5. Briel, D.; Drößler, K.; Rybak, A.; Holzer, M.; Dobner, B.
    Protected Mercaptoalkyl-pyrimidinones: Synthesis and Test for Immunostimulating Activity.
    Pharmazie 2005, 60, 415.

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2004

  1. Daub, K., Habermann, B.; Hahn, T.; Teich, L.;Eger, K.
    Synthesis of 3-Aryloxy-2-iodoemodines by Oxidation of Emodin with (Diacetoxyiodo)arenes.
    Eur. J. Organic Chemistry 2004, 4, 894.
  2. Briel, D.
    A New Synthesis of Thiazole Derivatives via Ring Transformation of 6-Imino-6H-1, 3-thiazine Hydroperchlorate.
    Heterocycles 2004, 63, 2319.

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2003

  1. Briel, D.
    Ring Transformation Reactions Starting from 6-Imino-6H-1,3-thiazines.
    Heterocycles 2003, 60, 2273.
  2. Briel, D.
    A New Synthesis of Pyrido[1,2-a]thieno[3,2-d]pyrimidines.
    Pharmazie 2003, 58, 836.
  3. Briel, D.; Holzer, M.; Leistner, S.; Drößler, K.; Dobner, B.
    Synthesis of Methylsulfanylpyrimidines with Immunomodulatory Activity.
    Pharmazie 2003, 58, 759.
  4. Dannat, K.; Tillner, J.; Winckler, T.; Weiss, M.; Eger, K.; Dingermann, T.
    Effects of medicinal compounds on the differentiation of the eukaryotic microorganism Dictyostelium discoideum: Can this model be used as a screening test for reproductive toxicity in humans?
    Pharmazie 2003, 58, 204.

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2002

  1. Kaap, S.; Quentin, l.;Tamiru, D.; Shaheen, M.; Eger, K.; Steinfelder, H. J.
    Structure activity analysis of the pro-apoptotic, anti-tumour effect of nitrostyrene adducts and related compounds.
    Biochem. Pharmacol. 2002, 65, 603.
  2. Habermann, B.; Schmidt, M.; Eger, K.
    Zink-Supplemente besser vor oder während der Mahlzeiten? Messungen der Komplexstabilitäten im System Zinkhistidin-Phytinsäure.
    Deutsche Lebensmittel-Rundschau     2002, 98, 295
  3. Briel, D.; Franz, T.; Dobner, B.
    Synthesis and Reactions of 6-Methylsulfanyl-2,4-dithioxo-1,2,3,4-tetrahydropyri-midin-5- carbonitrile.
    J. Heterocyclic Chem.     2002, 39, 863.
  4. Gütschow, M.; Hauschildt, S.; Benard, S.; Reichl, S.; Witt, U. G.; Eger, K.; Arnhold, J.;
    Michael adducts of palmitoyiascorbic acid: Effects on the oxidative burst of neutrophils and the production of TNF-alpha in monocytes.
    Pharmacology     2002, 66, 162.

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2001

  1. Hess, S.; Teubert, U.; Ortwein, J.; Eger, K.
    Profiling indomethacin impurities using high-performance liquid chromatography and nuclear magnetic resonance.
    Europ. J. Pharm. Sci. 2001, 301.
  2. Eschke, D.; Scheibler, P.; Hess, S.; Brand, A.; Eger, K.; Allgaier, C.; Nieber, K.
    Effects of a novel adenosine A1 receptor ligand on hypoxia induced changes of membrane properties and neurotransmitter releae in rat brain.
    Neurochem. Int. 2001, 391.
  3. Hess, S.; Dölker, M.; Haferburg, D.; Kertscher, H. P.; Matysik, F.-M.; Ortwein, J.; Teubert, U.; Zimmermann, W.; Eger, K.
    Separation, analyses and syntheses of trimethoprim impurities.
    Pharmazie 2001, 306.

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2000

  1. Gütschow, M.; Hecker,T.; Thiele, A.; Hauschildt, S.; Eger, K.
    Aza Analogues of Thalidomide: Synthesis and Evaluation as Inhibitors of Tumor Necrosis Factor-a Production In Vitro.
    Bioorg. Med Chem. 2000, 1059.
  2. Thiele, A.; Thormann, M.; Hofmann, H.-J.; Naumann,W. W.; Eger, K.; Hauschildt, S.
    A possible role of N-cadherin in thalidomide teratogenicity.
    Life Sciences 2000, 67, 457.

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1999

  1. Briel, D.; Pohlers, D.; Uhlig, M.; Vieweg, S.; Scholz, G.; Thormann, M.; Hofmann, H,J.
    3-Amino-5-phenoxythiophenes - A Novel Class of Inhibitors of the Cellular L-T3 Uptake.
    J. Med. Chem. 1999, 42, 1849.
  2. Briel, D.
    Intramolekulare ANRORC-Reaktion ausgehend von Pyrano[4,3-d]pyrimidinen - eine neue Methode zur Synthese von Thieno[2,3-d]pyrimidinen.
    Pharmazie 1999, 54, 858.

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Patente

  1. Sträter, N.; Zahn, M.; Nieber, K.; Erdmann, S.; Funke, U.; Scheunemann, M.; Fischer, S.; Brust, P.; Briel, D.; Schwan, G.; Kubicova, L.; Barbar Asskar, G.
    Neue Halogenalkoxychinazoline - deren Herstellung und Verwendung.
    Patent:DE 102010042833 (Deutschland) / WO 2012052556 (PCT-Anmeldung)
  2. Figg, W.; Eger, K.; Teubert, U.; Weiss, M.; Gütschow, M.; Hecker, T.;Hauschildt, S.
    Preparation of thalidomide metabolite analogs as potential angiogenesis inhibitors.
    Patent:WO 20020668414 (PCT-Anmeldung)
letzte Änderung: 30.10.2018