Medizinische Chemie

Antiinfektiva sind ein wichtiger Bestandteil der Behandlung von Infektionskrankheiten. Immer häufiger treten Krankheitserreger auf, die gegen viele Antibiotika resistent geworden sind - solche Infektionen sind dann nur schwer zu therapieren. Unsere Wissenschaftler bauen klassisch chemisch in Kolben mit Rührern, Heizpilzen und Kühlbädern neue Wirkstoffen nach dem Vorbild der Natur – um bakterielle Erkrankungen, Krebs und Parasiten-Infektionen wie Malaria in den Griff zu bekommen.

Publikationen

  • Essig,S.; Schmalzbauer,B.; Bretzke,S.; Scherer,O.; Koeberle,A.; Werz,O.; Müller,R.; Menche,D.; (2016). Predictive Bioinformatic Assignment of Methyl-Bearing Stereocenters, Total Synthesis, and an Additional Molecular Target of Ajudazol B. 81 4, 1333-1357 PubMed
  • Trenner,J.; Prusov,E.V.; (2015). A simple and efficient method for the preparation of 5-hydroxy-3-acyltetramic acids. 11, 323-327 DOI: 10.3762/bjoc.11.37 HZI-Repositorium PubMed
  • Zhang,S.; Schneider,L.S.; Vick,B.; Grunert,M.; Jeremias,I.; Menche,D.; Müller,R.; Vollmar,A.M.; Liebl,J.; (2015). Anti-leukemic effects of the V-ATPase inhibitor Archazolid A. 6 41, 43508-4352819492553 DOI: Article WEBURLS
  • Lu,H.H.; Hinkelmann,B.; Tautz,T.; Li,J.; Sasse,F.; Franke,R.; Kalesse,M.; (2015). Paleo-soraphens: Chemical total syntheses and biological studies. Organic and Biomolecular Chemistry: 13 29, 8029-803614770520 WEBURLS
  • Koutsoudakis,G.; Romero-Brey,I.; Berger,C.; Perez-Vilaro,G.; Perin,P.M.; Vondran,F.W.; Kalesse,M.; Harmrolfs,K.; Müller,R.; Martinez,J.P.; Pietschmann,T.; Bartenschlager,R.; Bronstrup,M.; Meyerhans,A.; Diez,J.; (2015). Soraphen A: a broad-spectrum antiviral natural product with potent anti-hepatitis C virus activity. 63 4, 813-821 DOI: 10.1016/j.jhep.2015.06.002 HZI-Repositorium PubMed
  • Bruns,N.; Collisi,W.; Bernecker,S.; Stadler,M.; Richter,C.; Schwalbe,H.; Kalesse,M.; (2015). Spirangien derivatives from the myxobacterium Sorangium cellulosum: Isolation, structure elucidation, and biological activity. European Journal of Organic Chemistry: 2015 4, 847-8571434193X
  • Herkommer,D.; Thiede,S.; Wosniok,P.R.; Dreisigacker,S.; Tian,M.; Debnar,T.; Irschik,H.; Menche,D.; (2015). Stereochemical determination of the leupyrrins and total synthesis of leupyrrin A<inf>1</inf>. Journal of the American Chemical Society: 137 12, 4086-408900027863 WEBURLS
  • Bluhm,N.; Kalesse,M.; (2015). Synthesis of a C20-Deoxygenated Spirangien Derivative for Target Identification. Synlett: 26 6, 797-80109365214
  • Naini,A.; Muthukumar,Y.; Raja,A.; Franke,R.; Harrier,I.; Smith,A.B.,III; Lee,D.; Taylor,R.E.; Sasse,F.; Kalesse,M.; (2015). The synthesis and biological evaluation of desepoxyisotedanolide and a comparison with desepoxytedanolide. 54 23, 6935-6939 PubMed
  • Niggemann,Jutta; Bozko,P.; Bruns,Nicole; Wodtke,Anne; Gieseler,M.T.; Thomas,K.; Jahns,C.; Nimtz,Manfred; Reupke,I.; Brüser,T.; Auling,G.; Malek,N.; Kalesse,Markus; (2014). Baceridin, a cyclic hexapeptide from an epiphytic bacillus strain, inhibits the proteasome. ChemBioChem: 15 7, 1021-102914397633 WEBURLS
  • Symkenberg,G.; Kalesse,Markus; (2014). Structure Elucidation and Total Synthesis of Kulkenon. Angewandte Chemie International Edition: 53 7, 1795-1798 PubMed
  • Tang,Wufeng; Liu,S.; Degen,D.; Ebright,R.H.; Prusov,Evgeny V.; (2014). Synthesis and Evaluation of Novel Analogues of Ripostatins. Chemistry - A European Journal: 20, 12310-12319 PubMed
  • Gieseler,M.T.; Kalesse,Markus; (2014). Synthesis of angiolam A. Organic Letters: 16 2, 548-551 PubMed
  • Hartmann,O.; Kalesse,Markus; (2014). The Structure Elucidation and Total Synthesis of beta-Lipomycin. Angewandte Chemie International Edition: 53 28, 7335-7338 PubMed
  • Kalesse,Markus; Cordes,M.; Symkenberg,G.; Lu,H.H.; (2014). The vinylogous Mukaiyama aldol reaction (VMAR) in natural product synthesis. Natural Products Reports: 31 4, 563-59414604752 WEBURLS
  • Irschik,H.; Washausen,Peter; Sasse,Florenz; Fohrer,J.; Huch,V.; Müller,Rolf; Prusov,Evgeny V.; (2013). Isolation, structure elucidation, and biological activity of maltepolides: remarkable macrolides from myxobacteria. Angewandte Chemie International Edition: 52 20, 5402-5405 WEBURLS
  • Lu,H.H.; Raja,A.; Franke,R.; Landsberg,D.; Sasse,Florenz; Kalesse,Markus; (2013). Synthesis and biological evaluation of paleo-soraphens. Angewandte Chemie Internationa Edition: 52 51, 13549-13552 PubMed
  • Rentsch,A.; Landsberg,D.; Brodmann,T.; Bulow,L.; Girbig,A.K.; Kalesse,Markus; (2013). Synthesis and Pharmacology of Proteasome Inhibitors. Angewandte Chemie International Edition: 52 21, 5450-5488 WEBURLS
  • Prusov,Evgeny V.; (2013). Synthesis of the spiroketal core of integramycin. Beilstein Journal of Organic Chemistry: 9, 2446-245018605397 DOI: 10.3762/bjoc.9.282 HZI-Repositorium PubMed
  • Borst,E.M.; Kleine-Albers,J.; Gabaev,I.; Babic,M.; Wagner,K.; Binz,A.; Degenhardt,I.; Kalesse,Markus; Jonjic,S.; Bauerfeind,R.; Messerle,M.; (2013). The human cytomegalovirus UL51 protein is essential for viral genome cleavage-packaging and interacts with the terminase subunits pUL56 and pUL89. Journal of Virology: 87 3, 1720-1732 DOI: 10.1128/JVI.01955-12 HZI-Repositorium PubMed
  • Prusov,Evgeny V.; (2013). Total synthesis of antibiotics: recent achievements, limitations, and perspectives. Applied in Microbiology and Biotechnology: 97 7, 2773-2795 DOI: 10.1007/s00253-013-4757-5 HZI-Repositorium PubMed
  • Diaz,N.; Zhu,M.; Ehrlich,G.; Eggert,U.; Muthukumar,Y.; Sasse,Florenz; Kalesse,Markus; (2012). An improved route to (+)-tedanolide and analysis of its subtle effects controlling conformation and biological behaviour. Chemistry: 18 16, 4946-4952 PubMed
  • Jahns,C.; Hoffmann,T.; Muller,S.; Gerth,Klaus; Washausen,Peter; Hofle,G.; Reichenbach,H.; Kalesse,Markus; Müller,Rolf; (2012). Pellasoren: Structure Elucidation, Biosynthesis, and Total Synthesis of a Cytotoxic Secondary Metabolite from Sorangium cellulosum. Angewandte Chemie International Edition: 51 21, 5239-5243 PubMed
  • Zander,W.; Irschik,H.; Augustiniak,H.; Herrmann,M.; Jansen,R.; Steinmetz,H.; Gerth,Klaus; Kessler,W.; Kalesse,Markus; Hofle,G.; Müller,Rolf; (2012). Sulfangolids, Macrolide Sulfate Esters from Sorangium cellulosum. Chemistry: 18 20, 6264-6271 PubMed
  • Diaz,N.; Naini,A.; Muthukumar,Y.; Sasse,Florenz; Kalesse,Markus; (2012). Synthesis of simplified tedanolide analogues-connecting tedanolide to myriaporone and gephyronic Acid. ChemMedChem: 7 5, 771-775 PubMed
  • Rentsch,A.; Kalesse,Markus; (2012). The total synthesis of corallopyronin a and myxopyronin b. Angewandte Chemie International Edition: 51 45, 11381-11384 PubMed
  • Tang,W.; Prusov,E.V.; (2012). Total synthesis of ripostatin a. Organic Letters: 14 17, 4690-4693 PubMed
  • Tang,W.; Prusov,E.V.; (2012). Total Synthesis of RNA-Polymerase Inhibitor Ripostatin B and 15-Deoxyripostatin. Angewandte Chemie International Edition: 51 14, 3401-3404 PubMed
  • Menche,D.; Li,P.; Irschik,Herbert*; (2010). Design, synthesis and biological evaluation of simplified analogues of the RNA polymerase inhibitor etnangien. Bioorganic and Medicinal Chemistry Letters: 20 3, 939-941 PubMed
  • Stauch,B.; Simon,B.; Basile,T.; Schneider,G.; Malek,N.P.; Kalesse,Markus*; Carlomagno,T.; (2010). Elucidation of the structure and intermolecular interactions of a reversible cyclic-peptide inhibitor of the proteasome by NMR spectroscopy and molecular modeling. Angewandte Chemie International Edition: 49 23, 3934-3938 PubMed
  • Kena,Diba A.; Noll,C.; Richter,M.; Gieseler,M.T.; Kalesse,Markus*; (2010). Intramolecular stereoselective protonation of aldehyde-derived enolates. Angewandte Chemie International Edition: 49 45, 8367-8369 PubMed
  • Brodmann,T.; Janssen,D.; Sasse,Florenz*; Irschik,Herbert*; Jansen,Rolf*; Müller,Rolf*; Kalesse,Markus*; (2010). Isolation and synthesis of chivotriene, a chivosazole shunt product from Sorangium cellulosum. European Journal of Organic Chemistry: 27, 5155-5159 DOI: 10.1002/ejoc.201000781
  • Niggemann,Jutta*; Gerth,Klaus*; Horstmann,N.; Bauerochse,A.; Kalesse,Markus*; (2010). Kultivierung und Identifizierung des endophytischen Pilzes Penicillium janthinellum Biourge aus dem Großen Moor bei Uchte (Niedersachsen) und Charakterisierung eines sekundären Stoffwechselproductes. Telma: 40, 245-254
  • Mohamed,I.E.; Kehraus,S.; Krick,A.; Konig,G.M.; Kelter,G.; Maier,A.; Fiebig,H.H.; Kalesse,Markus*; Malek,N.P.; Gross,H.; (2010). Mode of action of epoxyphomalins A and B and characterization of related metabolites from the marine-derived fungus Paraconiothyrium sp. Journal of Naturald Products: 73 12, 2053-2056 DOI: 10.1021/np100310k HZI-Repositorium PubMed
  • Li,P.; Li,J.; Arikan,F.*; Ahlbrecht,W.; Dieckmann,M.; Menche,Dirk*; (2010). Stereoselective total synthesis of etnangien and etnangien methyl ester. Journal of Organic Chemistry: 75 8, 2429-2444 DOI: 10.1021/jo100201f HZI-Repositorium PubMed
  • Bulow,L.; Nickeleit,I.; Girbig,A.K.; Brodmann,T.; Rentsch,A.; Eggert,U.; Sasse,Florenz*; Steinmetz,Heinrich*; Frank,Ronald*; Carlomagno,T.; Malek,N.P.; Kalesse,Markus*; (2010). Synthesis and biological characterization of argyrin F. ChemMedChem: 5 6, 832-836 PubMed
  • Rand,K.; Noll,C.; Schiebel,H.M.; Kemken,D.; Dulcks,T.; Kalesse,Markus*; Heinz,Dirk W.*; Layer,G.; (2010). The oxygen-independent coproporphyrinogen III oxidase HemN utilizes harderoporphyrinogen as a reaction intermediate during conversion of coproporphyrinogen III to protoporphyrinogen IX. Biological Chemistry: 391 1, 55-63 PubMed
  • Schackel,R.; Hinkelmann,B.; Sasse,Florenz*; Kalesse,Markus*; (2010). The synthesis of novel disorazoles. Angewandte Chemie International Edition: 49 9, 1619-1622 PubMed
  • Brodmann,T.; Janssen,D.; Kalesse,Markus*; (2010). Total synthesis of chivosazole F. Journal of the American Chemical Society: 132 39, 13610-13611 PubMed
  • Li,J.; Li,P.; Menche,Dirk*; (2009). An efficient procedure for the direct nucleophilic substitution of the abiko-masamune auxiliary. Synlett: 15, 2417-2420
  • Li,J.; Menche,Dirk*; (2009). Direct methods for stereoselective polypropionate synthesis: A survey. Synthesis: 14, 2293-2315
  • Hagelüken,G.; Albrecht,S.C.; Steinmetz,Heinrich*; Jansen,Rolf*; Heinz,Dirk W.*; Kalesse,Markus*; Schubert,Wolf-Dieter*; (2009). The absolute configuration of rhizopodin and its inhibition of actin polymerization by dimerization. Angewandte Chemie International Edition: 48 3, 595-598 PubMed
  • Li,P.; Li,J.; Arikan,F.; Ahlbrecht,W.; Dieckmann,M.; Menche,Dirk*; (2009). Total synthesis of etnangien. Journal of the American Chemical Society: 131 33, 11678-11679 PubMed
  • Nickeleit,I.; Zender,S.; Sasse,Florenz*; Geffers,Robert*; Brandes,G.; Sorensen,I.; Steinmetz,Heinrich*; Kubicka,S.; Carlomagno,T.; Menche,D.; Gutgemann,I.; Buer,J.; Gossler,A.; Manns,M.P.; Kalesse,Markus*; Frank,Ronald*; Malek,N.P.; (2008). Argyrin a reveals a critical role for the tumor suppressor protein p27(kip1) in mediating antitumor activities in response to proteasome inhibition. 14 1, 23-35 PubMed
  • Eggert,U.; Diestel,R.; Sasse,Florenz*; Jansen,Rolf*; Kunze,Brigitte*; Kalesse,Markus*; (2008). Chondramide C: Synthesis, configurational assignment, and structure-activity relationship studies. Angewandte Chemie - International Edition: 47 43, 6478-6482
  • Liang,J.; Ke,G.; You,W.; Peng,Z.; Lan,J.; Kalesse,Markus*; Tartakoff,A.M.; Kaplan,F.; Tao,T.; (2008). Interaction between importin 13 and myopodin suggests a nuclear import pathway for myopodin. Molecular and Cellular Biochemistry: 307 1-2, 93-100 PubMed
  • Lorenz,M.; Kalesse,Markus*; (2008). Synthesis of the C10-C32 core structure of spirangien A. Organic Letters: 10 19, 4371-4374 PubMed
  • Rahn,N.; Kalesse,Markus*; (2008). The total synthesis of chlorotonil A. Angewandte Chemie International Edition: 47 3, 597-599 PubMed
  • Janssen,D.; Albert,D.; Jansen,Rolf*; Müller,Rolf*; Kalesse,Markus*; (2007). Chivosazole A - elucidation of the absolute and relative configuration. Angewandte Chemie - International Edition: 46 26, 4898-4901 DOI: 1002/anie.200605198
  • Frank,Ronald*; Gerth,Klaus*; Kalesse,Markus*; Menche,Dirk*; Bilitewski,Ursula*; (2007). The chemical pipeline - a research program and infrastructure for the discovery and evaluation of new anti-infectives.: HZI Research Report 2006/2007. Jonas,Rainer; Schlender,Hannes; Braun,Manfred; (Ed.). Braunschweig : Helmholtz Centre for Infection Research GmbH (HZI), 32-43

Leitung

  • Prof. Dr. Markus Kalesse

    Argyrin Forschergruppe Argyrin Forschergruppe, Argyrin blockiert die molekulare Maschinerie der Zelle, mit der sie Proteine abbaut, die nicht mehr benötigt werden“, erklärt Malek, „und damit…

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Audio Podcast

  • Medizinische Chemie
    Medikamente wachsen nicht auf Bäumen oder im Boden. Oder vielleicht doch? Viele Bakterien produzieren Stoffe, die uns helfen könnten: Naturstoffe. Jutta Niggemann und Markus Kalesse versuchen aus diesen Naturstoffen neue Medikamente zu machen. Begleiten Sie beide ins Labor...