Participation in the Cluster of Excellence

CiM Principal Investigator
Coordinator Research Area C
Executive Board Member
Scientific Steering Committee Member
CiM-IMPRS Graduate School Member

Research Area A.5: Surface-Targeted Tracking of Individual Cells In Vivo
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)

© Westfälische Nachrichten - Jürgen Peperhowe

Podcast: Inflammation in the Brain

Imaging to Investigate Multiple Sclerosis

As the reasons for multiple sclerosis (MS) are yet not known, Prof. Lydia Sorokin and Prof. Günter Haufe cooperate in a project where they want to bring the progress of MS in sudden inflammatory attacks on pictures. Therefore, they improve and specifiy the method of molecular imaging - this research promises new understanding of the nervous disease MS. Listen here


  • 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


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, 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


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


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


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