Publikationen & Patente

Publikationen & Patente
2019
- Krieger, V.; Hamacher, A.; Cao, F.; Stenzel, K.; Gertzen, C. G. W.; Schäker-Hübner, L.; Kurz, T.; Gohlke, H.; Dekker, F. J.; Kassack, M. U.*, Hansen, F. K.* "Synthesis of peptoid-based class I selective histone deacetylase inhibitors with chemosensitizing properties" J. Med. Chem. 2019, 62, 11260-11279.
- Koehne, E.; Kreidenweiss, A.; Zoleko Manego, R.; McCall, M.; Mombo-Ngoma, G.; Mackwitz, M. K. W.; Hansen, F. K.; Held, J. "Histone Deacetylase Inhibitors with High In Vitro Activities Against Plasmodium falciparum Isolates Collected from Gabonese Children and Adults" Sci. Rep. 2019, 9:17336.
- Raudszus, R.; Nowothy, R.; Gertzen, C. G. W.; Schöler, A.; Krizsan, A.; Gockel. I.; Kalwa, H.; Gohlke, H.; Thieme, R.; Hansen, F. K. "Fluorescent analogs of peptoid-based HDAC inhibitors: synthesis, biological activity and cellular uptake kinetics" Bioorg. Med. Chem. 2019, DOI:10.1016/j.bmc.2019.07.055.
- Erdeljac, N.; Bussman, K.; Schöler, A.; Hansen, F. K.; Gilmour, R. "Fluorinated Analogues of the HDAC Inhibitor Vorinostat (Zolinza): Validation of a Chiral Hybrid Bioisostere of the Trifluoromethyl and Ethyl groups (BITE)" ACS Med. Chem. Lett. 2019, 10, 1336-1340.
- 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 ß-peptoid-capped HDAC inhibitors with anti-neuroblastoma and anti-glioblastoma activity" MedChemComm 2019, DOI: 10.1039/C8MD00454D.
- Mackwitz, M. K. W; Hesping, E.; Antonova-Koch, Y.; Diedrich, D.; Gebru, T.; Skinner-Adams, T.; Clarke, M.; Schöler, A.; Limbach, L; Kurz, Th.; Winzeler, E. A.; Held, J.; Andrews, K. T.; Hansen, F. K. "Structure-Activity and Structure-Toxicity Relationships of Novel Peptoid Based Histone Deacetylase Inhibotors with Dual-Stage Antiplasmodial Activity" ChemMedChem 2019, 14, 912-926.
2018
- 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 - 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. - 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. - 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.
- 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. - 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
- 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. - 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. - 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. - 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. - 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. - 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.
2014
- Burda, E.; Rademann, J.
Catalytic activation of pre-substrates via dynamic fragment assembly on protein templates.
Nature Comm. 2014, 5, 517. - 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. - 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.
2013
- 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. - 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. - 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. - 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.
2012
- 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.
2010
- Briel, D.; Rudolph, I.; Unverferth, K.
Synthesis of disubstituted 1,4-diazepines as potential benzodiazepine agonists.
Pharmazie 2010, 65, 641. - 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. - 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.
2009
- Briel, D.; Askar, G.B; Ortwein, J.; Unverferth, K.
A convenient synthesis of furans using bromacetylpyran-2-one.
Pharmazie 2009, 64, 477. - 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.
2008
- Rybak, A.; Kronbach, C.; Unverferth, K.; Briel, D.
Thieno[2,3-d]pyrimidines as Abtagonists of the Glutamate Receptors.
Pharmazie 2008, 63, 823.
2007
- 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.
2005
- 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. - 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. - Briel, D.
Synthesis and Conversion of 3-(2-Hydroxythiobenzamido)benzo[b]furans.
Heterocycles 2005, 65, 1295. - Briel, D.
Synthesis of Thieno[2,3-d]pyrimidines from 6-Imino-6H-1,3-thiazine Hydroperchlorates.
Pharmazie 2005, 60, 75. - Briel, D.; Drößler, K.; Rybak, A.; Holzer, M.; Dobner, B.
Protected Mercaptoalkyl-pyrimidinones: Synthesis and Test for Immunostimulating Activity.
Pharmazie 2005, 60, 415.
2004
- 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. - Briel, D.
A New Synthesis of Thiazole Derivatives via Ring Transformation of 6-Imino-6H-1, 3-thiazine Hydroperchlorate.
Heterocycles 2004, 63, 2319.
2003
- Briel, D.
Ring Transformation Reactions Starting from 6-Imino-6H-1,3-thiazines.
Heterocycles 2003, 60, 2273. - Briel, D.
A New Synthesis of Pyrido[1,2-a]thieno[3,2-d]pyrimidines.
Pharmazie 2003, 58, 836. - Briel, D.; Holzer, M.; Leistner, S.; Drößler, K.; Dobner, B.
Synthesis of Methylsulfanylpyrimidines with Immunomodulatory Activity.
Pharmazie 2003, 58, 759. - 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.
2002
- 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. - 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 - 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. - 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.
2001
- 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. - 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. - 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.
2000
- 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. - 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.
1999
- 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. - 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.
Patente
- 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) - 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)