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-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

2017

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, 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