Participation in “Cells in Motion”

  • Supervisor in the CiM-IMPRS Graduate Programme
  • Project FF-2015-03: CCR6 as a marker of CD4+Th17+ T cells in inflammation: development of specific imaging and therapeutic tools (Günter Haufe, Lydia Sorokin, project time: 07/2015 - 06/2017)
  • Project FF-2013-28: Development of novel, dual purpose, MOBSAM-based, specific inhibitors for MMP-2/9 to image and investigate their activity in inflammatory pathologies in vivo (Lydia Sorokin, Günter Haufe, project time: 07/2013 - 06/2015)
  • Patents

    • Chen G, Gangadharmath UB, Kasi D, Kolb HC, Liu C, Sinha A, Szardenings AK, Walsh JC, Wang E, Yu C, Zhang W, Kopka K, Haufe G, Schäfers M, Hugenberg V, Wagner S, Hermann S, Breyholz H-J, Faust A. Compounds with matrix-metalloproteinase inhibitory activity and imaging agents thereof. EP 2644601; 02/10/2013.
    • Haufe G, Schilson S, Keul P, Levkau B, Schäfers M. New ligands for targeting of S1P receptors for in vivo imaging and treatment of diseases. EP 2559683; 20/02/2013. WO 2013/026765; 28/02/2013. EP 2744776; 25/06/2014.
    • Haufe G, Hermann S, Hugenberg V, Kolb H, Kopka K, Wagner S, Schäfers M. Compounds with matrix-metalloproteinase inhibitory activity. WO 2013/010573; 24/01/2013.
    • Behrends M, Breyholz H-J, Hermann S, Haufe G, Hugenberg V, Kolb H, Kopka K, Wagner S, Schäfers M. Compounds with matrix-metalloproteinase inhibitory activity. EP 2520573; 07/11/2012.

  • CiM Papers

    2018

    Beutel B, Song J, Konken CP, Korpos E, Schinor B, Gerwien H, Vidyadharan R, Burmeister M, Li L, Haufe G, Sorokin L. New in Vivo Compatible Matrix Metalloproteinase (MMP)-2 and MMP-9 Inhibitors. Bioconjug Chem 2018;29: 3715-3725. Abstract
    Dreier A-L, Matsnev AV, Thrasher JS, Haufe G. Syn-selective silicon Mukaiyama-type aldol reactions of (pentafluoro-lambda(6)-sulfanyl)acetic acid esters with aldehydes. Beilstein J Org Chem 2018;14: 373-380. Abstract
    Hohn M, Chang M, Meisel JE, Frost E, Schwegmann K, Hermann S, Schäfers M, Riemann B, Haufe G, Breyholz HJ, Wagner S. Synthesis and preliminary in vitro and in vivo evaluation of thiirane-based slow binding MMP inhibitors as potential radiotracers for PET imaging. Chemistry Select 2018;3: 11729-11736. Abstract
    Hugenberg V, Behrends M, Wagner S, Hermann S, Schafers M, Kolb HC, Szardenings K, Walsh JC, Gomez LF, Kopka K, Haufe G. Synthesis, radiosynthesis, in vitro and first in vivo evaluation of a new matrix metalloproteinase inhibitor based on gamma-fluorinated alpha-sulfonylaminohydroxamic acid. EJNMMI Radiopharm Chem 2018;3: 10. Abstract

    2017

    Bartels K, Schinor B, Haufe G. Diastereoselectivity of cyclopropanation of substituted α-fluorostyrenes versus styrenes by different methods. Journal of Fluorine Chemistry 2017;203: 200-205. Abstract
    Borrello MT, Schinor B, Bartels K, Benelkebir H, Pereira S, Al-Jamal WT, Douglas L, Duriez PJ, Packham G, Haufe G, Ganesan A. Fluorinated tranylcypromine analogues as inhibitors of lysine-specific demethylase 1 (LSD1, KDM1A). Bioorg Med Chem Lett 2017;27: 2099-2101. Abstract
    Dreier A-L, Beutel B, Muck-Lichtenfeld C, Matsnev AV, Thrasher JS, Haufe G. Synthesis of alpha-(Pentafluorosulfanyl)- and alpha-(Trifluoromethyl)-Substituted Carboxylic Acid Derivatives by Ireland-Claisen Rearrangement. J Org Chem 2017;82: 1638-1648. Abstract
    Feskov IO, Chernykh AV, Kondratov IS, Klyachina M, Daniliuc CG, Haufe G. Cyclobutyl-Containing Rigid Analogues of Threonine: Synthesis and Physical Chemical Properties. J Org Chem 2017;82: 12863-12868. Abstract
    Kondratov IS, Logvinenko IG, Tolmachova NA, Morev RN, Kliachyna MA, Clausen F, Daniliuc CG, Haufe G. Synthesis and physical chemical properties of 2-amino-4-(trifluoromethoxy)butanoic acid - a CF3O-containing analogue of natural lipophilic amino acids. Org Biomol Chem 2017;15: 672-679. Abstract
    Ortmeyer CP, Haufe G, Schwegmann K, Hermann S, Schafers M, Borgel F, Wunsch B, Wagner S, Hugenberg V. Synthesis and evaluation of a [18F]BODIPY-labeled caspase-inhibitor. Bioorg Med Chem 2017;25: 2167-2176. Abstract

    2016

    Beutel B, Daniliuc CG, Riemann B, Schafers M, Haufe G. Fluorinated matrix metalloproteinases inhibitors-Phosphonate based potential probes for positron emission tomography. Bioorg Med Chem 2016;24: 902-909. Abstract
    Chernykh AV, Feskov IO, Chernykh AV, Kondratov IS, Tolmachova N, Radchenko DS, Daniliuc CG, Haufe G. Synthesis and Physical-Chemical Properties of cis- and trans-1-Amino-3-fluoro-3-methylcyclobutanecarboxylic Acids. Eur. J. Org. Chem. 2016;2016: 4782-4786. Abstract
    Friese FW, Dreier A-L, Matsnev AV, Daniliuc CG, Thrasher JS, Haufe G. Anti-Selective Aldol Reactions of Pentafluorosulfanylacetic Acid Esters with Aldehydes Mediated by Dicyclohexylchloroborane. Org Lett 2016;18: 1012-1015. Abstract
    Ramb DC, Lerchen A, Kischkewitz M, Beutel B, Fustero S, Haufe G. Addition of Nucleophiles to Fluorinated Michael Acceptors. Eur. J. Org. Chem. 2016;2016: 1751-1759. Abstract
    Ulbrich D, Daniliuc CG, Haufe G. Synthesis of alpha,omega-polyfluorinated alpha-amino acid derivatives and delta,delta-difluoronorvaline. Org Biomol Chem 2016;14: 2755-2767. Abstract
    Ulbrich D, Daniliuc CG, Haufe G. Halofluorination of N-protected α,β-dehydro-α-amino acid esters—A convenient synthesis of α-fluoro-α-amino acid derivatives. Journal of Fluorine Chemistry 2016;188: 65-75. Abstract

    2015

    Behrends M, Wagner S, Kopka K, Schober O, Schafers M, Kumbhar S, Waller M, Haufe G. New matrix metalloproteinase inhibitors based on gamma-fluorinated alpha-aminocarboxylic and alpha-aminohydroxamic acids. Bioorg Med Chem 2015;23: 3809-3818. Abstract
    Chernykh AV, Radchenko DS, Chernykh AV, Kondratov IS, Tolmachova NA, Datsenko OP, Kurkunov MA, Zozulya SX, Kheylik YP, Bartels K, Daniliuc CG, Haufe G. Synthesis and Physicochemical Properties of 3-Fluorocyclobutylamines: Synthesis and Properties of 3-Fluorocyclobutylamines. Eur. J. Org. Chem. 2015;2015: 6466-6471. Abstract
    Fustero S, Simon-Fuentes A, Barrio P, Haufe G. Olefin metathesis reactions with fluorinated substrates, catalysts, and solvents. Chem Rev 2015;115: 871-930. Abstract
    Kondratov IS, Bugera MY, Tolmachova NA, Posternak GG, Daniliuc CG, Haufe G. Radical Reactions of Alkyl 2-Bromo-2,2-difluoroacetates with Vinyl Ethers: "Omitted" Examples and Application for the Synthesis of 3,3-Difluoro-GABA. J Org Chem 2015;80: 12258-12264. Abstract
    Kondratov IS, Tolmachova NA, Dolovanyuk VG, Gerus II, Daniliuc C-G, Haufe G. Synthesis of Trifluoromethyl-Containing Polysubstituted Aromatic Compounds by Diels-Alder Reaction of Ethyl 3-Benz­amido-2-oxo-6-(trifluoromethyl)-2_H_-pyran-5-carboxylate: Trifluoromethyl-Containing Polysubstituted Aromatic Compounds. Eur. J. Org. Chem. 2015;2015: 2482-2491. Abstract
    Limpachayaporn P, Schafers M, Haufe G. Isatin sulfonamides: potent caspases-3 and -7 inhibitors, and promising PET and SPECT radiotracers for apoptosis imaging. Future Med Chem 2015;7: 1173-1196. Abstract
    Schilson SS, Keul P, Shaikh RS, Schafers M, Levkau B, Haufe G. Synthesis of new ligands for targeting the S1P1 receptor. Bioorg Med Chem 2015;23: 1011-1026. Abstract
    Shaikh RS, Keul P, Schäfers M, Levkau B, Haufe G. New fluorinated agonists for targeting the sphingosin-1-phosphate receptor 1 (S1P1). Bioorganic & Medicinal Chemistry Letters 2015;25: 5048-5051. Abstract
    Shaikh RS, Schilson SS, Wagner S, Hermann S, Keul P, Levkau B, Schafers M, Haufe G. Synthesis and evaluation of fluorinated fingolimod (FTY720) analogues for sphingosine-1-phosphate receptor molecular imaging by positron emission tomography. J Med Chem 2015;58: 3471-3484. Abstract
    Waldmann CM, Hermann S, Faust A, Riemann B, Schober O, Schafers M, Haufe G, Kopka K. Novel fluorine-18 labeled 5-(1-pyrrolidinylsulfonyl)-7-azaisatin derivatives as potential PET tracers for in vivo imaging of activated caspases in apoptosis. Bioorg Med Chem 2015;23: 5734-5739. Abstract

    2014

    Alsibai W, Hahnenkamp A, Eisenblatter M, Riemann B, Schafers M, Bremer C, Haufe G, Holtke C. Fluorescent Non-peptidic RGD Mimetics with High Selectivity for alphaVbeta3 vs alphaIIbbeta3 Integrin Receptor: Novel Probes for in Vivo Optical Imaging. J Med Chem 2014;57: 9971-9982. Abstract
    Gerling UIM, Salwiczek M, Cadicamo CD, Erdbrink H, Czekelius C, Grage SL, Wadhwani P, Ulrich AS, Behrends M, Haufe G, Koksch B. Fluorinated amino acids in amyloid formation: a symphony of size, hydrophobicity and α-helix propensity. Chem Sci 2014: 819-830. Abstract
    Limpachayaporn P, Wagner S, Kopka K, Schober O, Schafers M, Haufe G. Synthesis of 7-halogenated isatin sulfonamides: nonradioactive counterparts of caspase-3/-7 inhibitor-based potential radiopharmaceuticals for molecular imaging of apoptosis. J Med Chem 2014;57: 9383-9395. Abstract
    Prasad VP, Wagner S, Keul P, Hermann S, Levkau B, Schafers M, Haufe G. Synthesis of fluorinated analogues of sphingosine-1-phosphate antagonists as potential radiotracers for molecular imaging using positron emission tomography. Bioorg Med Chem 2014;22: 5168-5181. Abstract

    2013

    Limpachayaporn P, Riemann B, Kopka K, Schober O, Schäfers M, Haufe G. Influence of 4- or 5-substituents on the pyrrolidine ring of 5-[1-(2-methoxymethylpyrrolidinyl)sulfonyl]isatin derivatives on their inhibitory activities towards caspases-3 and -7. Eur J Med Chem 2013;64C: 562-578. Abstract
    Limpachayaporn P, Schäfers M, Schober O, Kopka K, Haufe G. Synthesis of new fluorinated, 2-substituted 5-pyrrolidinylsulfonyl isatin derivatives as caspase-3 and caspase-7 inhibitors: Nonradioactive counterparts of putative PET-compatible apoptosis imaging agents. Bioorg Med Chem 2013;21: 2025-2036. Abstract
    Limpachayaporn P, Wagner S, Kopka K, Hermann S, Schäfers M, Haufe G. Synthesis, 18F-radiolabeling, and in vivo biodistribution studies of N-fluorohydroxybutyl isatin sulfonamides using positron emission tomography. J Med Chem 2013;56: 4509-4520. Abstract
    Schinor B, Wibbeling B, Haufe G. Synthesis and pKa values of 2-(3- and 4-pentafluorosulfanylphenyl)-2-fluorocyclopropylamines. J Flourine Chem 2013: 102-109. Abstract

    2012

    Hugenberg V, Haufe G. Fluoro-Pummerer rearrangement and analogous reactions. J Fluorine Chem 2012;143: 238-262. Abstract
    Schrigten D, Breyholz HJ, Wagner S, Hermann S, Schober O, Schäfers M, Haufe G, Kopka K. A new generation of radiofluorinated pyrimidine-2,4,6-triones as MMP-targeted radiotracers for positron emission tomography. J Med Chem 2012: 223-232. Abstract