Publications of Institute of Radiopharmaceutical Cancer Research

74 Publications

2020

Deuteration versus ethylation – strategies to improve the metabolic fate of a 18F-labeled celecoxib derivative

Laube, M.; Gassner, C.; Neuber, C.; Wodtke, R.; Ullrich, M.; Haase-Kohn, C.; Löser, R.; Köckerling, M.; Kopka, K.; Knieß, T.; Hey-Hawkins, E.; Pietzsch, J.


2019

Introduction of the New Center for Radiopharmaceutical Cancer Research at Helmholtz-Zentrum Dresden-Rossendorf

Kreller, M.; Pietzsch, H.-J.; Walther, M.; Tietze, H.; Kaever, P.; Knieß, T.; Füchtner, F.; Steinbach, J.; Preusche, S.


Synthesis and cyclooxygenase inhibition of sulfonamide-substituted (dihydro)pyrrolo[3,2,1-hi]indoles and their potential prodrugs

Laube, M.; Gassner, C.; Knieß, T.; Pietzsch, J.


Nitric oxide-releasing selective estrogen receptor modulators (NO-SERMs): a bifunctional approach to improve the therapeutic index

Bechmann, N.; Knieß, T.; Pietzsch, J.


Fluorescent Mouse Pheochromocytoma Spheroids Expressing Hypoxia-Inducible Factor 2 alpha: Morphologic and Radiopharmacologic Characterization

Seifert, V.; Liers, J.; Kniess, T.; Richter, S.; Bechmann, N.; Feldmann, A.; Bachmann, M.; Eisenhofer, G.; Pietzsch, J.; Ullrich, M.


Fluorine-18 labeling of S100 proteins for small animal positron emission tomography

Laube, M.; Kniess, T.; Neuber, C.; Haase-Kohn, C.; Pietzsch, J.


Synthesis and preliminary radiopharmacological characterisation of an 11C-labelled azadipeptide nitrile as potential PET tracer for imaging of cysteine cathepsins

Laube, M.; Frizler, M.; Wodtke, R.; Neuber, C.; Belter, B.; Kniess, T.; Bachmann, M.; Gütschow, M.; Pietzsch, J.; Löser, R.

  • Open Access Logo Journal of Labelled Compounds and Radiopharmaceuticals 62(2019)8, 448-459
    DOI: 10.1002/jlcr.3729

One-pot Cascade Synthesis of Pyrazole-based Isosteres of Valdecoxib by a [3+2] Cycloaddition/[1,5] Sigmatropic Rearrangement Sequence and Evaluation of their COX Inhibitory Activity

Roscales, S.; Bechmann, N.; Pietzsch, J.; Kniess, T.


Access to 18F-labelled isoxazoles by Ruthenium-promoted 1,3-dipolar cycloaddition of 4-[18F]fluoro-N-hydroxybenzimidoyl chloride with alkynes.

Roscales, S.; Kniess, T.

  • Open Access Logo Journal of Labelled Compounds and Radiopharmaceuticals 62(2019), 393-403
    DOI: 10.1002/jlcr.3708

2018

Bridging from Brain to Tumor imaging: (S)- and (R)-[18F]Fluspidine for investigation of Sigma-1 Receptors in Tumor-bearing Mice

Kranz, M.; Bergmann, R.; Kniess, T.; Belter, B.; Neuber, C.; Cai, Z.; Deng, G.; Fischer, S.; Steinbach, J.; Zhou, J.; Huang, H.; Brust, P.; Deuther-Conrad, W.; Pietzsch, J.


Evaluation of fluorine-18-labelled alpha1(I)-N-telopeptide analogues as substrate-based radiotracers for PET imaging of melanoma-associated lysyl oxidase

Kuchar, M.; Neuber, C.; Belter, B.; Bergmann, R.; Lenk, J.; Wodtke, R.; Kniess, T.; Steinbach, J.; Pietzsch, J.; Löser, R.


Novel Valdecoxib Derivates by Ruthenium-catalyzed 1,3-Dipolar Cycloaddition of Nitrile Oxides with Alkynes - Synthesis and COX-2 Inhibition Affinity.

Roscales, S.; Bechmann, N.; Weiss, D. H.; Köckerling, M.; Pietzsch, J.; Kniess, T.


2017

Nitric oxide-releasing selective cyclooxygenase-2 inhibitors as promising radiosensitizers in melanoma cells in vitro

Bechmann, N.; Hauser, S.; Hofheinz, F.; Kniess, T.; Pietzsch, J.

  • Open Access Logo Annals of Radiation Therapy and Oncology 1(2017)2, 1010

99mTechnetium-based Small Molecule Radiopharmaceuticals and Radiotracers Targeting Inflammation and Infection

Kniess, T.; Laube, M.; Wüst, F.; Pietzsch, J.


Development of Fluorinated Non-Peptidic Ghrelin Receptor Ligands for Potential Use in Molecular Imaging

Moldovan, R.-P.; Els-Heindl, S.; Worm, D. J.; Kniess, T.; Kluge, M.; Beck-Sickinger, A. G.; Deuther-Conrad, W.; Krügel, U.; Brust, P.


Hydrous 18F-fluoroethylation – leaving off the azeotropic drying

Kniess, T.; Laube, M.; Steinbach, J.


2016

Development of a F-18-labeled Diaryl-Substituted Dihydropyrrolo[3,2,1-hi]indole as Potential Probe for Functional Imaging of Cyclooxygenase-2 with PET

Gassner, C.; Neuber, C.; Laube, M.; Bergmann, R.; Kniess, T.; Pietzsch, J.


Development of antioxidant COX-2 inhibitors as radioprotective agents for radiation therapy – a hypothesis-driven review

Laube, M.; Kniess, T.; Pietzsch, J.


5-Chloro-1-phenylpentan-1-one

Bechmann, N.; Kniess, T.; Pietzsch, J.; König, J.; Köckerling, M.


2015

Protective effects of 2,3-diaryl-substituted indole-based cyclooxygenase-2 inhibitors on oxidative modification of human low density lipoproteins in vitro

Pietzsch, J.; Laube, M.; Bechmann, N.; Pietzsch, F.-J.; Kniess, T.

  • Open Access Logo Clinical Hemorheology and Microcirculation 61(2015)4, 615-632
    DOI: 10.3233/CH-141923

18F-Labeled 1,4-Dioxa-8-azaspiro[4.5]decane Derivative: Synthesis and Biological Evaluation of a σ1 Receptor Radioligand with Low Lipophilicity as Potent Tumor Imaging Agent

Xie, F.; Bergmann, R.; Kniess, T.; Deuther-Conrad, W.; Mamat, C.; Neuber, C.; Liu, B.; Steinbach, J.; Brust, P.; Pietzsch, J.; Jia, H.


2-[18F]Fluoroethyl tosylate - a versatile tool for building 18F-based radiotracers for positron emission tomography

Knieß, T.; Laube, M.; Brust, P.; Steinbach, J.


Novel (pyrazolyl)benzenesulfonamides with a nitric oxide-releasing moiety as selective cyclooxygenase-2 inhibitors

Bechmann, N.; Kniess, T.; Köckerling, M.; Pigorsch, A.; Steinbach, J.; Pietzsch, J.


Novel indole-based sigma-2 receptor ligands: synthesis, structure–affinity relationship and antiproliferative activity

Xie, F.; Kniess, T.; Neuber, C.; Deuther-Conrad, W.; Mamat, C.; Liebermann, B. P.; Liu, B.; Mach, R. H.; Brust, P.; Steinbach, J.; Pietzsch, J.; Jia, H.


Optical imaging of COX-2: Studies on an autofluorescent 2,3-diaryl-substituted indole-based cyclooxygenase-2 inhibitor.

Tondera, C.; Ullm, S.; Laube, M.; Meister, S.; Neuber, C.; Mosch, B.; Kniess, T.; Pietzsch, J.


Diaryl-substituted (dihydro)pyrrolo[3,2,1-hi]indoles, a class of potent COX-2 inhibitors with tricyclic core structure

Laube, M.; Gassner, C.; Sharma, S. K.; Günther, R.; Pigorsch, A.; König, J.; Köckerling, M.; Wuest, F.; Pietzsch, J.; Kniess, T.


2014

Organotypical vascular model for characterization of radioprotective compounds: Studies on antioxidant 2,3-diaryl-substituted indole-based cyclooxygenase-2 inhibitors

Ullm, S.; Laube, M.; Bechmann, N.; Knieß, T.; Pietzsch, J.

  • Clinical Hemorheology and Microcirculation 58(2014), 281-295
    DOI: 10.3233/CH-141902

2,3-Diaryl-substituted indole based COX-2 inhibitors as leads for imaging tracer development

Laube, M.; Tondera, C.; Sharma, S. K.; Bechmann, N.; Pietzsch, F.-J.; Pigorsch, A.; Köckerling, M.; Wuest, F.; Pietzsch, J.; Kniess, T.


2013

Radiosynthesis and in vivo Evaluation of a 18F-Labelled Styryl-Benzoxazole Derivative for ß-Amyloid Targeting

Ribeiro Morais, G.; Kniess, T.; Bergmann, R.; Gano, L.; Abrunhosa, A.; Santos, I.; Paulo, A.


Radiolabeled COX-2 inhibitors for non-invasive visualization of COX-2 expression and activity - a critical update

Laube, M.; Kniess, T.; Pietzsch, J.


Investigations into the synthesis, radiofluorination and conjugation of a new [18F]fluorocyclobutyl prosthetic group and its in vitro stability using a tyrosine model system

Franck, D.; Kniess, T.; Steinbach, J.; Zitzmann-Kolbe, S.; Friebe, M.; Dinkelborg, L. M.; Graham, K.


Visualization of cyclooxygenase-2 using a 2,3-diarylsubstituted indole-based inhibitor and confocal laser induced cryofluorescence microscopy at 20 K in melanoma cells in vitro

Tondera, C.; Laube, M.; Wimmer, C.; Kniess, T.; Mosch, B.; Großmann, K.; Pietzsch, J.


2-Carbaborane-3-phenyl-1H-indoles—Synthesis via McMurry Reaction and Cyclooxygenase (COX) Inhibition Activity

Laube, M.; Neumann, W.; Scholz, M.; Lönnecke, P.; Crews, B.; Marnett, L. J.; Pietzsch, J.; Kniess, T.; Hey-Hawkins, E.


2012

Synthesis, in silico, in vitro, and in vivo investigation of 5-[11C]methoxy-substituted sunitinib, a tyrosine kinase inhibitor of VEGFR-2

Caballero, J.; Muñoz, C.; Alzate-Morales, J. H.; Cunha, S.; Gano, L.; Bergmann, R.; Steinbach, J.; Kniess, T.


Synthesis and cytotoxicity of pyridine and quinoline oxorhenium(V) complexes with tridentate (NS2, S-3)/monodentate (s) coordination

Segal, I.; Zablotskaya, A.; Kniess, T.; Shestakova, I.


Novel 7α-alkoxy-17α-(4’-halophenylethynyl)estradiols as potential SPECT/PET imaging agents for estrogen receptor expressing tumors: synthesis and binding affinity evaluation

Neto, C.; Oliveira, M. C.; Gano Fernanda Marques, M. L.; Yasuda, T.; Thiemann, T.; Kniess, T.; Santos, I.


Radioiodinated sunitinib as a potential radiotracer for imaging angiogenesis - radiosynthesis and first radiopharmacological evaluation of 5-[125I]Iodo-sunitinib

Kuchar, M.; Oliveira, M. C.; Gano, L.; Santos, I.; Knieß, T.


Radiohalogenated 4-anilinoquinazoline-based EGFR-TK inhibitors as potential cancer imaging agents

Neto, C.; Fernandes, C.; Oliveira, M. C.; Gano, L.; Mendes, F.; Kniess, T.; Santos, I.


Study of differences in the VEGFR2 inhibitory activities between semaxanib and SU5205 using 3D-QSAR, docking, and molecular dynamics simulations

Munoza, C.; Adasmea, F.; Alzate-Morales, J. H.; Vergara-Jaquea, A.; Kniess, T.; Caballero, J.


Radiolabeled small molecule inhibitors of VEGFR – recent advances

Kniess, T.


Site-selective radiolabeling of peptides by 18F-fluorobenzoylation with [18F]SFB in solution and on solid phase - a comparative study

Kuchar, M.; Pretze, M.; Knieß, T.; Steinbach, J.; Pietzsch, J.; Löser, R.


Radiosynthesis of a 18F-labeled 2,3-diarylsubstituted indole via McMurry coupling for functional characterization of cyclooxygenase-2 (COX-2) in vitro and in vivo

Kniess, T.; Laube, M.; Bergmann, R.; Graf, F.; Steinbach, J.; Wuest, F.; Pietzsch, J.


2011

Synthesis of an 18F-labeled cyclin-dependent kinase-2 inhibitor

Svensson, F.; Kniess, T.; Bergmann, R.; Pietzsch, J.; Wuest, F.

  • Journal of Labelled Compounds and Radiopharmaceuticals 54(2011), 769-774
    DOI: 10.1002/jlcr.1922

Radiolabeling of phosphatidylserine-binding peptides with prosthetic groups N-[6-(4-[18F]fluorobenzylidene)aminooxyhexyl]maleimide ([18F]FBAM) and N-succinimidyl-4-[18F]fluorobenzoate ([18F]SFB)

Kapty, J.; Kniess, T.; Wuest, F.; Mercer, J. R.


Synthesis and evaluation of 1,5-diaryl-substituted tetrazoles as novel selective cyclooxygenase-2 (COX-2) inhibitors

Al-Hourani, B. J.; Sharma, S. K.; Mane, J. Y.; Tuszynski, J.; Baracos, V.; Kniess, T.; Suresh, M.; Pietzsch, J.; Wuest, F.


Automated radiosynthesis of the thiol-reactive labeling agent N-[6-(4-[18F]fluorobenzylidene)aminooxyhexyl]maleimide ([18F]FBAM)

Knieß, T.; Kuchar, M.; Pietzsch, J.


2010

Synthesis of neurotensin(8-13)-phosphopeptide heterodimers via click chemistry

Richter, S.; Ramenda, T.; Bergmann, R.; Knieß, T.; Steinbach, J.; Pietzsch, J.; Wuest, F.


2009

Radiolabelling of proteins with fluorine-18 via click chemistry

Ramenda, T.; Knieß, T.; Bergmann, R.; Steinbach, J.; Wüst, F.


PET-Tracer für die onkologische Diagnostik: Welche radiomarkierten Substanzen sind relevant?

Knieß, T.; Steinbach, J.

  • Onkologische Pharmazie 11(2009)4, 4-5

Synthesis and radiopharmacological investigation of 3-[4’-[18F]fluorobenzylidenyl]-indolin-2-one as possible tyrosine kinase inhibitor

Knieß, T.; Bergmann, R.; Kuchar, M.; Steinbach, J.; Wüst, F.


Synthesis and cyclooxygenase inhibition of various (aryl-1,2,3-triazole-1-yl)-methanesulfonylphenyl derivatives

Wuest, F.; Tang, X.; Knieß, T.; Pietzsch, J.; Suresh, M.


Radiosynthesis and radiopharmacological evaluation of [N-methyl-11C]Org 34850 as a glucocorticoid receptor (GR)-binding radiotracer

Wüst, F.; Knieß, T.; Henry, B.; Peeters, B. W. M. M.; Wiegerinck, P. H. G.; Pietzsch, J.; Bergmann, R.


Cell cycle regulating kinase Cdk4 as a potential target for tumor cell treatment and tumor imaging

Graf, F.; Köhler, L.; Knieß, T.; Wüst, F.; Mosch, B.; Pietzsch, J.


2008

Synthesis and evaluation in vitro and in vivo of a 11C-labeled cyclooxygenase-2 (COX-2) inhibitor

Wüst, F.; Knieß, T.; Bergmann, R.; Pietzsch, J.


Facile synthesis of various nitro-substituted derivatives of semaxinib (SU 5416)

Knieß, T.; Kuchar, M.; Wüst, F.


Radiolabeled glucocorticoids as molecular probes for imaging brain glucocorticoid receptors by means of positron-emission-tomography (PET)

Steiniger, B.; Knieß, T.; Bergmann, R.; Pietzsch, J.; Wüst, F.

  • Mini-Reviews in Medicinal Chemistry 8(2008)7, 728-739

Practical experiences with the synthesis of [11C]CH3 trough gas phase iodination reaction using a TRACERlabFXC synthesis module

Knieß, T.; Rode, K.; Wüst, F.


2007

Synthesis and radiopharmacological characterization of [11C]AL-438 as a nonsteroidal ligand for imaging brain glucocorticoid receptors

Wüst, F.; Knieß, T.; Bergmann, R.; Henry, B.; Pietzsch, J.

  • Bioorganic & Medicinal Chemistry Letters 17(2007), 4035-4039

2005

Synthesis and radiopharmacological evaluation of 2´-(4-fluorophenyl)-21-[18F]fluoro-20-oxo-11β,17α-dihydroxy-pregn-4-eno[3,2-c]pyrazole as potential glucocorticoid receptor ligand for positron emission tomography (PET)

Wüst, F.; Knieß, T.; Kretzschmar, M.; Bergmann, R.

  • Bioorganic & Medicinal Chemistry Letters 15(2005), 1303-1306

Synthesis and biological evaluation of S-[11C]methylated mercaptoimidazolde piperazinyl derivatives as potential radioligands for imaging 5-HT1A receptors by positron emission tomography (PET)

Garcia, R.; Xavier, C.; Paulo, A.; Santos, I.; Knieß, T.; Bergmann, R.; Wüst, F.

  • Journal of Labelled Compounds and Radiopharmaceuticals 48(2005), 301-315

N-Arylation of indoles with 4-[18F]fluoroiodobenzene: synthesis of 18F-labelled σ2 receptor ligands for positron emission tomography (PET)

Wüst, F.; Knieß, T.

  • Journal of Labelled Compounds and Radiopharmaceuticals 48(2005), 31-43
    DOI: 10.1002/jlcr.893

2004

Synthesis and biological evaluation of silylated mixed-ligand 99mTc complexes with the [PNS/S] donor atom set

Fernandes, C.; Knieß, T.; Gano, L.; Seifert, S.; Spies, H.; Santos, I.


No-carrier added synthesis of 18F-labelled nucleosides using Stille cross-coupling reactions with 4-[18F]fluoroiodobenzene

Wüst, F.; Knieß, T.

  • Journal of Labelled Compounds and Radiopharmaceuticals 47(2004), 457-468
    DOI: 10.1002/jlcr.834

2003

Synthesis and Enzymatic Evaluation of Nucleosides Derived from 5-Iodo-2'-deoxyuridines

Knieß, T.; Grote, M.; Noll, B.; Johannsen, B.

  • Z. Naturforsch. 58b, 226-230 (2003)

Silylated mixed-ligand rhenium complexes with the [PNS/S] donor atom set

Knieß, T.; Fernandes, C.; Santos, I.; Kraus, W.; Spies, H.

  • Inorganica Chimica Acta 348 (2003) 237-241

Synthesis of 4-[18F]fluoroiodobenzene and its application in Sonogashira cross-coupling reactions

Wüst, F.; Knieß, T.

  • Journal of Labelled Compounds and Radiopharmaceuticals 2003, 46: 699-713
  • Lecture (Conference)
    15th International Symposium on Radiopharmaceutical Chemistry; Sydney, 07.-18.08.2003.

2002

Synthesis and biological activity of ‚3+1' mixed ligand (3-thiapentane-1,5-dithiolato)oxorhenium(V) complexes bearing 1,2,3,4-tetrahydro(iso)quinoline and quinoline

Zablotskaya, A.; Segal, I.; Germane, S.; Shestakova, I.; Lukevics, E.; Knieß, T.; Spies, H.

  • Applied Organometallic Chemistry 16 (2002) 550-555

Synthesis of hydroxyl silylated rhenium and (99mTc)technetium ‚3+1'mixed ligand complexes

Knieß, T.; Spies, H.; Santos, I.; Zablotskaya, A.

  • J Label Compd Radiopharm 45 (2002) 629-636

2001

Synthesis and physico-chemical characterization of triorganylsiloxyalkyl monodentate ligands with free mercapto group.

Zablotskaya, A.; Segal, I.; Lukevics, E.; Knieß, T.; Spies, H.

  • Latv. Kim. Z. N4 (2001) 339-342

1999

Nicotinamide-substituted complexes as redox markers. 2. Synthesis of a 99Tc-dihydropyridine mixed-ligand complex and investigation of the stability in tissue homogenates

Rother, A.; Kniess, T.; Pütz, M.; Jungclas, H.; Spies, H.; Johannsen, B.

  • Journal of Labelled Compounds and Radiopharmaceuticals 42, 673-681(1999)

Effective coupling of Re/Tc-MAG3 complexes with amines and nucleobases in aprotic solvents.

Kniess, T.; Noll, S.; Noll, B.; Spies, H.; Johannsen, B.

  • Journal of Radioanalytical and Nuclear Chemistry, 240, No. 2 (1999), 657-660

Nicotinamide-substituted complexes as redox markers 2. Synthesis of a 99Tc dihydropyridine mixed-ligand complex and investigation of the stability in tissue homogenates

Rother, A.; Knieß, T.; Pütz, M.; Jungclas, H.; Spies, H.; Johannsen, B.

  • J. Labelled Cpd. Radiopharm. 42 (1999) 673-681

1998

Nicotinamide-Substituted Complexes as Redox Marker

Knieß, T.; Spies, H.; Brandau, W.; Johannsen, B.

  • Journ. Labelled Comp. and Radiopharm. XLI, 605-614 (1998)

1996

Rhenium(V) gluconate, a suitable precursor for the preparation of rhenium(V) complexes

Noll, B.; Knieß, T.; Friebe, M.; Spies, H.; Johannsen, B.