Publikationen & Patente

2018

  1. 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, in press
  2. 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, DOI: 10.1021/acs.jmedchem.8b01013
  3. 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.
  4. Sanil Bhatia, Daniela Diedrich, Benedikt Frieg, Heinz Ahlert, Stefan Stein, Bertan Bopp, Franziska Lang, Tao Zang, Tobias Kroeger, Thomas Ernst, Gesine Koegler, Andreas Krieg, Steffen Luedeke, Hana Kunkel, Ana J. Rodrigues Moita, Matthias U. Kassack, Viktoria Marquardt, Friederike Opitz, Marina Oldenburg, Marc Remke, Florian Babor, Manuel Grez, Andreas Hochhaus, Arndt Borkhardt, Georg Groth, Luitgard Nagel-Steger, Joachim Jose, Thomas Kurz, Holger Gohlke, Finn K. Hansen* (co-senior author), Julia Hauer* 
    “Targeting HSP90 dimerization via the C-terminus is effective in imatinib resistant CML and lacks heat shock response” 
    Blood 2018, in press.

 

 

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: 07.09.2018