Publications

2020


Theo Rodat, Melanie Krebs, Alexander Döbber, Björn Jansen, Anja Steffen-Heins, Kathrin Schwarz, Christian Peifer.
Restricted suitability of BODIPY for caging in biological applications based on singlet oxygen generation. Photochemical & Photobiological Sciences 2020, https://doi.org/10.1039/D0PP00097C

Stefan Kirschner, Alexander Döbber, Melanie Krebs, Christopher Witt, Bernd Hartke and Christian Peifer. The Impact of electronic effects on photolysis: a model study on the 4,5-dimethoxy-2-nitrobenzyl caged N-phenylpyrimidine-2-amine scaffold. ChemPhotoChem 2020, 4, 1-7. doi.org/10.1002/cptc.201900285

2019


Congxing Liu, Lydia Witt, Chiara Ianes, Joachim Bischof, Marie-Thérèse Bammert, Joana Baier, Stefan Kirschner, Doris Henne-Bruns, Pengfei Xu, Marko Kornmann, Christian Peifer, Uwe Knippschild. Newly developed CK1-specific inhibitors show specifically stronger effects on CK1 mutants and colon cancer cell lines. Int. J. Mol. Sci. 2019, 20, 6184; doi:10.3390/ijms20246184

Fengjie Li, Christian Peifer, Dorte Janussen, Deniz Tasdemir. New Discorhabdin Alkaloids from the Antarctic Deep-Sea Sponge Latrunculia biformis. Mar. Drugs 2019, 17, 439 doi:10.3390/md17080439

Mark Hoorens, Maria Ourailidou, Theo Rodat, Petra van der Wouden, Piermichele Kobauri, Malte Kriegs, Christian Peifer, Ben Feringa, Frank Dekker, Wiktor Szymanski. Light-controlled Inhibition of BRAFV600E Kinase. European Journal of Medicinal Chemistry 2019, Volume 179, 133-146.

Zhigang Meng, Thomas Böhm, Pengfei Xu, Doris Henne-Bruns, Christian Peifer, Lydia Witt, Uwe Knippschild, and Joachim Bischof. CK1d kinase activity is modulated by PKCa by site-specific phosphorylation within the kinase domain of CK1d. Biochimica et Biophysica Acta (BBA) - Proteins and Proteomics BBA, 2019 Volume 1867, Issues 7–8, July–August 2019, Pages 710-721.

Miriam Schehr, Chiara Ianes, Jörn Weisner, Matthias P. Müller, Christian Pichlo, Julia Charl, Elena Brunstein, Linda Heintze, Julia Ewert, Marc Lehr, Ulrich Baumann, Daniel Rauh, Uwe Knippschild, Christian Peifer, and Rainer Herges. 2-Azo-, 2-diazocine-thiazols and 2-azo-imidazoles as photoswitchable kinase inhibitors: limitations and pitfalls of the photoswitchable inhibitor approach Photochemical & Photobiological Sciences, 2019, doi: 10.1039/C9PP00010K

Andreas Luxenburger, Dorian Schmidt, Chiara Ianes, Christian Pichlo, Marc Krüger, Thorsten von Drathen, Elena Brunstein, Graeme J. Gainsford, Ulrich Baumann, Uwe Knippschild and Christian Peifer. Design, synthesis and biological evaluation of isoxazole-based CK1 inhibitors modified with chiral pyrrolidine scaffolds. Molecules 2019, 24, 873; doi:10.3390/molecules24050873

Anna Laís Pfeifer Barbosa, Arlette Stenzel-Storjohann, Jose Diomedes Barbosa, Christian Zidorn, Christian Peifer, Deniz Tasdemir, and Serhat Sezai Cicek. Antimicrobial and cytotoxic effects of the Copaifera reticulata oleoresin and its main diterpene acids. Journal of Ethnopharmacology 233 (2019), 94–100.

2018


Dorian Schmidt, Theo Rodat, Linda Heintze, Jantje Weber, Rebecca Horbert, 
Ulrich GirreserTim Raeker, Lara Bußmann, Malte Kriegs, Bernd Hartke and 
Christian Peifer. 
Axitinib – A Photoswitchable Approved Tyrosine Kinase Inhibitor. ChemMedChem 2018 doi.org/10.1002/cmdc.201800531

Fengjie Li, Dorte Janussen, Christian Peifer, Ignacio Pérez-Victoria, Deniz Tasdemir. Targeted Isolation of Tsitsikammamines from the Antarctic Deep-sea Sponge Latrunculia biformis by Molecular Networking and Anticancer Activity. Mar. Drugs, 2018, 16 , 268 
doi:10.3390/md16080268.

Balbina García-Reyes, Lydia Witt, Björn Jansen, Ebru Karasu, Tanja Gehring, Johann Leban, Doris Henne-Bruns, Christian Pichlo, Elena Brunstein, Ulrich Baumann, Fabian Wesseler, Bernd Rathmer, Dennis Schade, Christian Peifer, and Uwe Knippschild. Discovery of Inhibitor of Wnt Production 2 (IWP-2) and Related Compounds As Selective ATP-Competitive Inhibitors of Casein Kinase 1 (CK1) δ/ε. J. Med. Chem., 2018, 61 (9), pp 4087–4102. 
doi:10.1021/acs.jmedchem.8b00095.

Christine Dolde, Simon Grüter, Joachim Bischof, Montada Anna, Jakob Halekotte, Christian Peifer, Hubert Kalbacher, Ulrich Baumann, Uwe Knippschild, and Beat Suter. A CK1 FRET biosensor reveals that DDX3X is an essential activator of CK1d&e. Journal of Cell Science (2018) 131, jcs207316. 
doi:10.1242/jcs.207316.

2017


Nadezhda A. Rupakova, Vasiliy A. Bakulev, Uwe Knippschild, Balbina García-Reyes, Oleg S. Eltsov, Grigoriy P. Slesarev, Nikolai Beliaev, Pavel A. Slepukhin, Lydia Witt, Christian Peifer, and Tetyana V. Beryozkina. Design and synthesis of N-benzimidazol-2-yl-N'-sulfonyl acetamidines. Archive for Organic Chemistry Arkivoc 2017, part iii, 225-240. 

Alexander Doebber, Athena F. Phoa, Brett W. Stringer, Bryan W. Day, Terrance G. Johns, Mohammed Abadleh, Christian Peifer, Lenka Munoz. Development and biological evaluation of a photoactivatable small molecule microtubule-targeting agent. ACS MedChemLett 2017, 8, 395-400. 
doi:10.1021/acsmedchemlett.6b00483

Jakob Halekotte, Lydia Witt, Chiara Ianes, Marc Krüger, Mike Bührmann,Daniel Rauh, Christian Pichlo, Elena Brunstein, Andreas Luxenburger,Ulrich Baumann, Uwe Knippschild, Joachim Bischof, and Christian Peifer. 
Optimized 4,5-Diaryl-imidazoles as Potent/Selective Inhibitors of Protein Kinase CK1δ and Their Structural Relation to p38α MAPK. Molecules 2017, 22(4), 522,
doi:10.3390/molecules22040522 

Karl J. Föhr, Uwe Knippschild, Anna Herkommer, Michael Fauler, Christian Peifer, Michael Georgieff, and Oliver Adolph. 
State-dependent block of voltage-gated sodium channels by the casein-kinase 1 inhibitor IC261. Invest New Drugs 2017, 1-13.
doi:10.1007/s10637-017-0429-0 

2016


Eugen Bethke, Boris Pinchuk, Christian Renn, Lydia Witt, Joachim Schlosser, and Christian Peifer. 
From type I to type II: design, synthesis and characterization of potent pyrazin-2-ones as DFG-out inhibitors of PDGFRβ. ChemMedChem, VIP article online Nov 2016,
doi:10.1002/cmdc.201600494 

Pinchuk, B., Horbert, R., Döbber, A., Kuhl, L, and Peifer, C. 
Photoactivatable Caged Prodrugs of VEGFR-2 Kinase Inhibitors. Molecules 2016, 21, 570,
doi:10.3390/molecules21050570 

2015


Phoaa, A.F., Browne, S., Gurgisa, F.M.S., Åkerfeldta, M.C., Döbber, A., Renn, C., Peifer, C., Stringer, B.W., Day, B.W., Wong, C., Chircop, M., Johns, T.G., Kassioug, M., Munoz, L. 
Pharmacology of novel small-molecule tubulin inhibitors in glioblastoma cells with enhanced EGFR signaling. Biochemical Pharmacology 2015,
doi:10.1016/j.bcp.2015.10.014

Zindler, M., Renn, C., Pinchuk, B., Horbert, R., Döbber, A., and Peifer, C. Design, synthesis and characterization of a photoactivatable caged prodrug of imatinib. ChemMedChem
doi: 10.1002/cmdc.201500163

Horbert, R., Pinchuk, B., Davies. P., Alessi, D. and Peifer, C. Photoactivatable prodrugs of anti-melanoma agent vemurafenib. ACS Chemical Biology doi:10.1021/acschembio.5b00174

Schlosser, J., Johannes, E., Zindler, M., Lemmerhirt, J., Sommer, B., Schütt, M., and Peifer, C. Novel synthesis of benzofuran- and indol-2-yl-methanamine derivatives. Tetrahedron Letters 2015, 56, 89–94.

Horbert, R., Pinchuk, B., Johannes, E., Schlosser, J., Schmidt, D., Cappel, D., Totzke, F., Schächtele, F., and Peifer, C. 
Optimization of Potent DFG-in Inhibitors of Plateled Derived Growth Factor Receptorβ (PDGF-Rβ) Guided by Water Thermodynamics.
J. Med. Chem. 2015, 58 (1), 170-182 (Special Issue: New Frontiers in Kinases. doi:10.1021/jm500373x).

2014


Richter, J., Ullah, K., Xu, P., Alscher, V., Blatz, A., Peifer, C., Halekotte, J., Leban, J., Vitt, D., Holzmann, K., Bakulev, V., Pinna, L., Henne-Bruns, D., Hillenbrand, A., Kornmann, M., Leithäuser, F., Bischof, J., and Knippschild, U. 
Effects of altered expression and activity levels of CK1δ and ε on tumor growth and survival of colorectal cancer patients. International Journal of Cancer 2014, in press

Knippschild, U., Krüger M., Richter J., Xu P., García-Reyes B., Peifer C., Halekotte J., Bakulev V. and Bischof, J. 
The CK1 family: contribution to cellular stress response and its role in carcinogenesis. Frontiers in Oncology 2014, 4:96.
doi:10.3389/fonc.2014.00096

2013


Pinchuk, B., Johannes, E., Gul, S., Schlosser, J., Schaechtele, C., Totzke, F., and Peifer, C. Marine derived Hamacanthins as lead for the development of novel PDGFRβ protein kinase inhibitors. Marine Drugs 2013, 11, 3209-3223; 
doi:10.3390/md11093209.

Johannes, E., Horbert, R., Schlosser, J., Schmidt, D., and Peifer, C. Effective synthesis of 3,5-diaryl-(1H)-pyrazin-2-ones via microwave mediated ring closure. Tetrahedron Letters 54(2013), 4067 – 4072.

2012


Knippschild, U., Peifer, C., Bischof, J., Kramer, K. Other tyrosine kinase inhibitors in development and future directions, in EMERGING TYROSINE KINASE INHIBITORS FOR GASTROINTESTINAL STROMAL TUMOR, edited by Dr. Peter Reichardt. Future Medicine, doi: 10.2217/EBO.12.16

Hirner, H., Günes, C.,Wolff, S., Bischof, J., Grothey, A., Oswald, F., Peifer, C., Kühl, M., Wegwitz, F., Bösl, M., Henne-Bruns, D., Leithäuser, F., Deppert, W., Knippschild, U. Impaired CK1 delta activity attenuates SV40-induced cellular transformation in vitro and mouse mammary carcinogenesis in vivo (2012). PLoS ONE 7(1): e29709. doi:10.1371/journal.pone.0029709

2010


Munoz, L., Ramsey, E., Manetsch, M., Ge, Qi, Peifer, C., Laufer, S., Ammit, J. A. Novel p38MAPK inhibitor ML3403 has potent anti-inflammatory activity in airway smooth muscle (2010). European Journal of Pharmacology, 635, 212-218.

Munoz, L., Selig, R., Yeung, Y. T., Peifer, C., Hauser, D., Laufer, S. Fluorescence polarisation binding assay to develop inhibitors of inactive p38alpha mitogen-activated protein kinase (2010). Analytical Biochemistry, 401, 125-133.

2009


Peifer, C., Abadleh, M., Hauser, D., Schattel, V., Hirner, H., Bischof, J., Knippschild, U., and Laufer, S. 3,4-Diaryl-isoxazoles and -imidazoles as Potent Dual Inhibitors of p38α MAPK and CK1 (2009). J. Med. Chem. 52, 7618-7630.

Peifer, C., Bühler, S., Hauser, D., Kinkel, K., Totzke, F., Schächtele, C. and Laufer, S. Design, Synthesis and Characterization of N7/N9 substituted 6-Aminopurines as VEGF-R and EGF-R Inhibitors (2009). European Journal of Medicinal Chemistry 44, 1788-1793.

2008


Peifer, C., Selig, R., Kinkel, K., Ott, D., Totzke, F., Schächtele, C, Heidenreich, R., Röcken, M., Schollmeyer, D. and Laufer, S. Design, Synthesis and Biological Evaluation of Novel 3-aryl-4-(1H-indole-3yl)-1,5-dihydro-2H-pyrrole-2-ones as VEGF-R inhibitors (2008). J. Med. Chem. 51, 3814-3824.

Peifer, C., Urich, R., Schattel, V., Abadleh, M., Röttig, M., Kohlbacher, O. and Laufer, S. Implications for selectivity of 3,4-Diarylquinolinones as p38α MAP Kinase inhibitors (2008). Bioorg. Med. Chem. Letters 18, 1431-1435.

Peifer, C., Alessi, D.R. (2008): New anti- cancer role for PDK1 inhibitors: Preventing resistance to tamoxifen. Biochemical Journal 417, 5-7.

Peifer, C., Alessi, D.R. Small Molecule Inhibitors of PDK1 (2008). ChemMedChem 3, 1810-1838.

2007


Peifer, C., Kinkel, K., Abadleh, M., Schollmeyer, D. and Laufer, S. (2007): From five to six membered rings: 3,4-Diarylchinolinone as lead for novel p38MAP kinase inhibitors. J. Med. Chem. 50, 1213-1221.

Peifer, C., Troschütz, R. (2007): Oxacillin-Natrium-Monohydrat. Arzneibuch-Kommentar zum EuAB/DAB, 25. Aktualisierung.

Buehler, S., Schollmeyer, D., Hauser, D., Laufer, S. and Peifer, C. (2007): 2-(6-Amino-7H-purine-7-yl)-1-phenylethanone. Acta Cryst. E63, 4646-4647.

Buehler, S., Schollmeyer, D., Hauser, D., Laufer, S. and Peifer, C. (2007): 2-(6-Methoxy-7H-purine-7-yl)-1-phenylethanone. Acta Cryst. E63, 4154-4155.

Peifer, C., Schollmeyer, D., Kinkel, K. and Laufer, S. (2007): 3-(4-Fluorophenyl)-1-methyl-4-pyridin-4-ylquinolin-2(1H)-one. Acta Cryst. E63, 2457-2459.

Peifer, C., Schollmeyer, D., Tschertsche, M. and Laufer, S. (2007): (2aRS,3RS,4aSR,6aRS,6bSR)-3-Hydroxy-2a,3,4a,6,6a,6b-hexahydro-1,4-dioxacyclopenta[cd]pentalen-2(5H)-one. Acta Cryst. E63, 2249-2251.

Kinkel, K., Laufer, S, Schollmeyer, D. and Peifer, C. (2007): 2,2-Dimethyl-N-[3-(3,4,5-trimethoxybenzoyl)pyridin-4-yl]propanamide. Acta Cryst. E63, 1887-1889.

Peifer, C., Schollmeyer, D., Tschertsche, M. and Laufer, S. (2007): rac-(3E, 3aR, 6aR)-3-(Hydroxymethylene)-3,3a,6,6a-tetrahydro-2H-cyclopenta[b]furan-2-one. Acta Cryst. E63, 1551-1553.

Abadleh, M., Peifer, C., Kinkel, K., Schollmeyer, D. and Laufer, S. (2007): 4-(5-(4-Fluorophenyl)-3-isopropylisoxazol-4-yl)pyridin-2(1H)-one. Acta Cryst. E63, 1423-1425.

Peifer, C., Ott, D., Schollmeyer, D. and Laufer, S. (2007): Ethyl 2,3-dihydro-1H,1'H-2,3'-biindol-1-yl(oxo)acetate. Acta Cryst. E63, 1415-1417.

Peifer, C., Selig, R., Schollmeyer, D. and Laufer, S. (2007): N-(2-[1-(Triisopropylsilyl)-1H-indol-3-yl]-2-[(triisopropylsilyl)oxy]vinyl)-2-(3,4,5-trimethoxyphenyl)acetamide. Acta Cryst. E63, 1266-1268.

2006


Peifer, C., Krasowski, A., Hämmerle, N., Kohlbacher, O., Dannhardt, G., Totzke, F., Schächtele, C. and Laufer, S. (2006): Profile and Molecular Modeling of 3-(Indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole-2,5-dione (1) as a Highly Selective VEGF-R2/3 Inhibitor. J. Med. Chem. 49, 7549-7553.

Peifer, C., Luik, S., Thuma, S., Herweh, Y. and Laufer, S. (2006): Development and Optimization of a Non-Radioactive JNK3 Assay. Combinatorial Chemistry & High Throughput Screening, 9 (8), 613-618.

Peifer, C., Stoiber, T., Unger, E., Totzke, F., Schächtele, C., Marmé, D., Brenk, R., Klebe, G., Schollmeyer, D., Dannhardt, G. (2006): Design, Synthesis and Biological Evaluation of 3,4-Bisarylmaleimides as Angiogenesis Inhibitors. J. Med. Chem. 49(4), 1271-1281.

Peifer, C., Wagner, G., Laufer, S. (2006): New Approaches to the Treatment of Inflammatory Disorders Small Molecule inhibitors of p38 MAP Kinase. Curr. Top. Med. Chem. 6(2), 113-49.

Peifer, C., Schollmeyer, D., Selig, R. and Laufer, S. (2006): 4-(4-Fluorophenyl)-3-(4-pyridin)quinolin-2(1H)-one. Acta Cryst., E62, 2648-2650.

Peifer, C., Laudage, S., Schollmeyer, D. and Laufer, S. (2006): 3-(4-Fluorophenyl)-4-pyridin-4-ylquinolin-2(1H)-one. Acta Cryst., E62, 2475-2477.

Peifer, C., Werz, O., Poeckel, D., Schollmeyer, D. and Laufer, S. (2006): (4R)-4-hydroxy-1-[(2S)-2-hydroxydodecyl]-L-proline monohydrate. Acta Cryst. E62, 5138-5140.

Peifer, C., Abadleh, M., Schollmeyer, D. and Laufer, S. (2006): 3,4-bis(4-fluorophenyl)-1,2,5-oxadiazole 2-oxide. Acta Cryst. E62, 4827-4828.

Peifer, C., Abadleh, M., Schollmeyer, D. and Laufer, S. (2006): 4-[3-(4-Fluorophenyl)-5-isopropylisoxazol-4-yl]pyridine. Acta Cryst. E62, 3707-3709.

Peifer, C., Abadleh, M., Schollmeyer, D. and Laufer, S. (2006): 5-(4-Fluorophenyl)-3-isopropylisoxazol-4-yl]-pyridine. Acta Cryst. E62, 3647-3649.

2005


Laufer, S., Thuma, S., Peifer, C., Greim, C., Herweh, Y., Albrecht, A. and Dehner, F. (2005): An immunosorbent, non radioactive p38 MAP kinase assay comparable to standard radioactive liquid phase assays. Analytical Biochemistry 344, 135-137.

Schollmeyer, D., Kammerer, B., Peifer, C. and Laufer, S. (2005): 3(RS)-Bromo-3-[1(SR)-phenyl-propyl]-chroman-2,4-dione. Acta Cryst. E61, 868-869.

Schollmeyer, D., Peifer, C. and Dannhardt, G. (2005): (3-Methanesulfonyloxy-4-methoxy-phenyl)-oxo-acetic acid methyl ester. Acta Cryst. E61, 583-584.

Schollmeyer, D., Peifer C. and Dannhardt, G. (2005): 3-(3,4,5-Trimethoxyphenyl)-4-(3-hydroxy-4-methoxyphenyl)-1H-pyrrole-2,5-dione. Acta Cryst. E61, 604-606.

Peifer, C., Schollmeyer, D. and Dannhardt, G. (2005): 3-(Indole-3-yl)-4-(3,4,5-trimethoxyphenyl)-1H-pyrrole-2,5-dione. Acta Cryst. E61, 721-723.

Peifer, C., Schollmeyer, D. and Dannhardt, G. (2005): 5,6,7-Trimethoxy-1,2,3,8-tetrahydro-benzo[a]pyrrolo[3,4-c]carbazole-1,3-dione containing one equivalent of DMSO. Acta Cryst. E61, 724-725.

2004


Peifer, C. and Dannhardt, G. (2004): A Novel Quantitative Chick Embryo Assay as an Angiogenesis Model Using Digital Image Analysis. Anticancer Res. 24(3a), 1545-51.

Peifer, C., Hofner A.F. (2004): Angiogenesis inhibition: New strategy in tumor therapy (Angiogenesehemmung: Neue Strategien in der Tumortherapie). Titelbeitrag der Pharmazeutischen Zeitung Volume 149, Issue 33, Pages 14-21.