Preclinical lead optimization of a 1, 2, 4-triazole based tankyrase inhibitor J Waaler, RGG Leenders, ST Sowa, S Alam Brinch, M Lycke, P Nieczypor, ... Journal of Medicinal Chemistry 63 (13), 6834-6846, 2020 | 34 | 2020 |
Chlorodifluoromethyl-substituted monosaccharide derivatives—radical activation of the carbon–chlorine-bond A Wegert, M Hein, H Reinke, N Hoffmann, R Miethchen Carbohydrate research 341 (16), 2641-2652, 2006 | 23 | 2006 |
Development of a 1, 2, 4-triazole-based lead tankyrase inhibitor: part II RGG Leenders, SA Brinch, ST Sowa, E Amundsen-Isaksen, A Galera-Prat, ... Journal of Medicinal Chemistry 64 (24), 17936-17949, 2021 | 19 | 2021 |
Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective κ-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo M Soeberdt, P Molenveld, RPM Storcken, R Bouzanne des Mazery, ... Journal of Medicinal Chemistry 60 (6), 2526-2551, 2017 | 19 | 2017 |
Structure–Activity Relationship Studies on (R)‐PFI‐2 Analogues as Inhibitors of Histone Lysine Methyltransferase SETD7 DC Lenstra, E Damen, RGG Leenders, RH Blaauw, FPJT Rutjes, ... ChemMedChem 13 (14), 1405-1413, 2018 | 16 | 2018 |
One-Pot synthesis of trifluoromethylated pyrazol-4-yl-pyrrole-2, 5-dione derivatives F Yuan, W Duan, Z Li, X Luo, M Zhang, H Deng, L Song Synthesis 51 (17), 3345-3355, 2019 | 14 | 2019 |
Methylation of geometrically constrained lysine analogues by histone lysine methyltransferases AHK Al Temimi, PB White, MJM Mulders, NGA van der Linden, ... Chemical Communications 56 (20), 3039-3042, 2020 | 12 | 2020 |
Examining sterically demanding lysine analogs for histone lysine methyltransferase catalysis AHKA Temimi, V Tran, RS Teeuwen, AJ Altunc, HIV Amatdjais-Groenen, ... Scientific Reports 10 (1), 3671, 2020 | 10 | 2020 |
Quantitative assessment of drug delivery to tissues and association with phospholipidosis: a case study with two structurally related diamines in development I Loryan, E Hoppe, K Hansen, F Held, A Kless, K Linz, V Marossek, ... Molecular Pharmaceutics 14 (12), 4362-4373, 2017 | 10 | 2017 |
The tankyrase inhibitor OM-153 demonstrates antitumor efficacy and a therapeutic window in mouse models SA Brinch, E Amundsen-Isaksen, S Espada, C Hammarström, ... Cancer Research Communications 2 (4), 233-245, 2022 | 9 | 2022 |
Synthesis of 2, 3-or 1, 2-unsaturated derivatives of 2-deoxy-2-trifluoromethylhexopyranoses A Wegert, H Reinke, R Miethchen Carbohydrate research 339 (10), 1833-1837, 2004 | 9 | 2004 |
Organofluorine compounds and fluorinating agents, Part 33: Regioselective chlorodifluoromethylations in the 1-position of 1, 2-unsaturated monosaccharide derivatives A Wegert, R Miethchen, M Hein, H Reinke Synthesis 2005 (11), 1850-1858, 2005 | 6 | 2005 |
3-(carboxyethyl)-8-amino-2-oxo-1, 3-diaza-spiro-[4.5]-decane derivatives S Kuehnert, RM Koenigs, F Jakob, A Kless, A Wegert, P Ratcliffe, ... | 5 | 2020 |
3-(Carboxymethyl)-8-Amino-2-Oxo-1, 3-Diaza-Spiro-[4.5]-Decane Derivatives S Kuehnert, RM Koenigs, F Jakob, A Kless, P Ratcliffe, R Jostock, T Koch, ... US Patent App. 15/405,919, 2017 | 5 | 2017 |
3-((Hetero-) Aryl)-8-Amino-2-Oxo-1, 3-Diaza-Spiro-[4.5]-Decane Derivatives S Kuehnert, RM Koenigs, A Kless, A Wegert, I Konetzki, P Ratcliffe, ... US Patent App. 15/405,485, 2017 | 5 | 2017 |
3-((Hetero-) Aryl)-Alkyl-8-Amino-2-Oxo-1, 3-Diaza-Spiro-[4.5]-Decane Derivatives S Kuehnert, RM Koenigs, A Kless, A Wegert, P Ratcliffe, R Jostock, ... US Patent App. 15/405,896, 2017 | 5 | 2017 |
8-Amino-2-Oxo-1, 3-Diaza-Spiro-[4.5]-Decane Derivatives S Kuehnert, RM Koenigs, A Kless, A Wegert, P Ratcliffe, R Jostock, ... US Patent App. 15/405,627, 2017 | 5 | 2017 |
Synthesis of a thymidine-derived acylsilane: A new synthetic intermediate towards thymidine analogues A Wegert, JB Behr, N Hoffmann, R Miethchen, C Portella, ... Synthesis 2006 (14), 2343-2348, 2006 | 5 | 2006 |
3-(carboxymethyl)-8-amino-2-oxo-1, 3-diaza-spiro-[4.5]-decane derivatives S Kuehnert, RM Koenigs, F Jakob, A Kless, P Ratcliffe, R Jostock, T Koch, ... US Patent App. 16/212,723, 2019 | 4 | 2019 |
3-((Hetero-) Aryl)-8-Amino-2-Oxo-1, 3-Diaza-Spiro-[4.5]-Decane Derivatives S Kuehnert, R Koenigs, A Kless, A Wegert, I Konetzki, P Ratcliffe, ... US Patent App. 16/207,854, 2019 | 4 | 2019 |