Martin-Luther-Universität Halle-Wittenberg

Publikationen 2017

Weitere Informationen zu den Publikationen der AG Prof. Sippl finden sie hier:

T. Heimburg, F. R. Kolbinger, P. Zeyen, E. Ghazy, D. Herp, K. Schmidtkunz, J. Melesina, T. B. Shaik, F. Erdmann, M. Schmidt, C. Romier, D. Robaa, O. Witt, I. Oehme, M. Jung, and W. Sippl. Structure-based design and biological characterization of selective HDAC8 inhibitors with anti-neuroblastoma activity. J. Med. Chem, in press DOI:10.1021/acs.jmedchem.7b01447   

L. Temme, B. Frehland, D. Schepmann, D. Robaa, W. Sippl, B. WünschHydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation Eur J Med Chem, in press doi:10.1016/j.ejmech.2017.12.054   

J. Schulz-Fincke, M. Hau, J. Barth, D. Robaa, D. Willmann, A. Kürner, J. Haas, G. Greeve, T. Haydn, S. Fulda, E. Metzger, M. Lübbert, S. Lüdeke, T. Berg, W. Sippl, R. Schüle, and M. Jung. Structure-Activity Studies on N-Substituted Tranylcypromine Derivatives Lead to Selective Structure-activity studies on N -Substituted tranylcypromine derivatives lead to selective inhibitors of lysine specific demethylase 1 (LSD1) and potent inducers of leukemic cell differentiation. Eur. J. Med. Chem, 144 (2018) 52e67. doi.org/10.1016/j.ejmech.2017.12.001   

M. Schmidt , A. Rohe, C. Platzer, A. Najjar, F. Erdmann, and W. Sippl. Regulation of G2/M transition by inhibition of WEE1 and PKMYT1 kinases. Molecules, 22(12), pii: E2045, 2017. doi:10.3390/molecules22122045   

M. Wünsch, J. Senger, P. Schultheisz, S. Schwarzbich, K. Schmidtkunz, C. Michalek, M. Klaß, S. Goskowitz ,P.  Borchert , L. Praetorius, W. Sippl , M. Jung, N. Sewald.Structure-Activity Relationship of Propargylamine-Based HDAC Inhibitors.ChemMedChem. 2017 Nov 9. doi:10.1002/cmdc.201700550   .

T. Fischer, A. Najjar, F. Totzke, C. Schächtele, W. Sippl , C. Ritter, A. Hilgeroth. Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and PDGFR-β related to anticancer drug resistance. J Enzyme Inhib Med Chem. 2018 Dec;33(1):1-8. doi:10.1080/14756366.2017.1370583   

A. C. Mora Huertas, C. E. H. Schmelzer, C. Luise, W. Sippl, M. Pietzsch, W. Hoehenwarter, A. Heinz. Degradation of tropoelastin and skin elastin by neprilysin. Biochimie, in press  doi.org/10.1016/j.biochi.2017.11.018

S. Swyter, M. Schiedel, D. Monaldi, A. Lehotzky, T. Rumpf, J. Ovádi, W. Sippl, M. Jung. New chemical tools for probing activity and inhibition of the NAD+ dependent lysine deacylase sirtuin. Philosophical Transactions B, in press

S. Gawaskar, L. Temme, J. A. Schreiber, D. Schepmann, A. Bonifazi, D. Robaa, W. Sippl, N. Strutz-Seebohm, G. Seebohm, B. Wünsch. Design, synthesis, pharmacological evaluation and docking studies of novel GluN2B selective NMDA receptor antagonists with benzo[7]annulen-7-amine scaffold. ChemMedChem 12(15):1212-1222. doi:10.1002/cmdc.201700311   

M. Schiedel, D. Herp, S. Hammelmann, S. Swyter, A. Lehotzky, D Robaa, J. Oláh, J. Ovádi, W. Sippl,  M. Jung. Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals). J. Med. Chem. 2017 Apr 17. doi:10.1021/acs.jmedchem.6b01872   . Commented in Science "In the Pipeline   ".

F. Ntie-Kang, K. K. Telukunt, K. Döring, C. V. Simoben, A. F. A. Moumbock, Y. I. Malange, L. E. Njume, J. N. Yong, W. Sippl, and S. Günther. NANPDB: A Resource for Natural Products from Northern African Sources. J. Nat. Prod. 80(7):2067-2076. DOI:10.1021/acs.jnatprod.7b00283   .

A. F.A. Moumbock, C. V. Simoben, L. Wessjohann, W. Sippl, S. Günther and F. Ntie‐Kang. Computational Studies and Biosynthesis of Natural Products with Promising Anticancer Properties. In: Medicine - Natural Products and Cancer Drug Discovery.    Ed. Farid A. BadriaIntech: ISBN 978-953-51-3314-8, Print ISBN 978-953-51-3313-1.

K. Stenzel, A. Chakrabarti, J. Melesina,  F. K. Hansen, J. Lancelot, S. Herkenhöhner, B. Lungerich, M. Marek, C. Romier, R. J. Pierce, W. Sippl, M. Jung, T. Kurz. Alkoxyamide-based HDAC Inhibitors as Potent Inhibitors of HDAC8 from Schistosoma mansoni. Archiv der Pharmazie, 2017 May 26. doi:10.1002/ardp.201700097   .

D. Wutz, D. Gluhacevic, A. Chakrabarti, K. Schmidtkunz, D. Robaa, F. Erdmann, C. Romier, W. Sippl, M. Jung, B. König. Photochromic histone deacetylase inhibitors based on dithienylethenes and fulgimides. Org Biomol Chem. 15(22):4882-4896, 2017. doi:10.1039/c7ob00976c.    

Moumbock, A. F. A.; Simoben, C. V.; Wessjohann, L.; Sippl, W.; Günther, S.; Ntie-Kang, F. Computational studies and biosynthesis of natural products with promising anticancer properties. In Phytochemistry - Natural Products and Cancer. Badria, F. A. (Editor). InTech: ISBN 978-953-51-5277-4.

A. Najjar, F. Ntie-Kang, W. Sippl. Application of computer modeling to anticancer natural products drug discovery. In Unique Aspects of Anti-cancer Drug Development. Latosińska, J.; Latosińska, M. (Editors); InTech: ISBN 978-953-51-5240-8

L. L. S. Scholte, M. M. Mourãa, F. Sviatopolk-Mirsky Paisa, J. Melesina, D. Robaa, A. C. Volpini, W. Sippl, R. J. Piercee, G. Oliveira, L. A. Nahum. Evolutionary relationships among protein lysine deacetylases of parasites causing neglected diseases, Infect Genet Evol. 53:175-188, 2017. doi:10.1016/j.meegid.2017.05.011   .

T. Fischer, T. Krüger, A. Najjar, F. Totzke, C. Schächtele, W. Sippl, C. Ritter, A. Hilgeroth. Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors. Bioorg Med Chem Lett. 27(12), 2708-2712, 2017. doi:10.1016/j.bmcl.2017.04.053.   

S. Vojacek, K. Beese, Z. Al Halabi, S. Swyter, A. Bodtke, C. Schulzke, M. Jung, W. Sippl, and A. Link. Three-Component Aminoalkylations Yielding Dihydronaphthoxazine-Based Sirtuin Inhibitors: Scaffold Modification and Exploration of Space for Polar Side-Chains. Arch Pharm (Weinheim). 2017 May 26. 350(7). doi:10.1002/ardp.201700097   .

G. S. Hailu, D. Robaa, M. Forgione, M.W. Sippl, D. Rotili, A. Mai. Potential of Histone Deacetylase Inhibitors as Anti-Parasitic Agents. J. Med. Chem. 60, 4780-4804, 2017. doi:10.1021/acs.jmedchem.6b01595   .

E. E. Gurda,l B. Turgutalp, H. O. Gulcan, T. Erçetin, M. F. Sahin, I.  Durmaz. R. C.  Atalay, Q. D.  Nguyen, W. Sippl. M. Yarim. Synthesis of Novel Benzothiazole-Piperazine Derivatives and Their Biological Evaluation as Acetylcholinesterase Inhibitors and Cytotoxic Agents. Anticancer Agents Med Chem. 2017 Apr 12. doi:10.2174/1871520617666170412153604.   

M. Schiedel, A. Fallarero, C. Luise, W. Sippl, P. Vuorela, and M. Jung. Synthesis and biological evaluation of 8-hydroxy-2,7-naphthyridinium salts as potent inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE). Med. Chem. Comm. 8, 465-470, 2017. DOI:10.1039/C6MD00647G   

C. Hempel, F. Totzke, C. Schaechtele, A. Najjar, W.  Sippl, C. Ritter, A. Hilgeroth. Discovery of novel dual inhibitors of receptor tyrosine kinases EGFR and IGF-1R. J. Enzyme Inhib. Med. Chem. 32, 271–276, 2017. doi:10.1080/14756366.2016.1247062   .

B. Sauer, T. S. Skinner-Adams, A. Bouchut, M. J. Chua, C. Pierrot, F. Erdmann, D. Robaa, M. Schmidt, J. Khalife, K. T. Andrews, W. Sippl Synthesis, biological characterisation and structure activity relationships of aromatic bisamidines active against Plasmodium falciparum. Eur. J. Med. Chem. 127, 22-40, 2017. doi:10.1016/j.ejmech.2016.12.041.   

F. Erdmann, W. Lin, C. Platzer, M Schmidt, W. Sippl, G. Fischer, Y. Zhang. Augmented Reversible Photoswitching of Drug-Target Interaction through "Surface Borrowing". Biochem Pharmacol.125, 84-92, 2017. doi:10.1016/j.bcp.2016.11.011   

M. Schiedel, D. Robaa, T. Rumpf, W. Sippl, M. Jung. The Current State of NAD+-Dependent Histone Deacetylases (Sirtuins) as Novel Therapeutic Targets. Med. Res. Rev. 38(1), 147-200, 2018. doi:10.1002/med.21436.   

D.Lehmann, L. Motlagh, D. Robaa, S. Zierz. Muscle Carnitine Palmitoyltransferase II Deficiency: A Review of Enzymatic Controversy and Clinical Features. Int. J. Mol. Sci.18, pii: E82, 2017. doi:10.3390/ijms18010082   

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