A novel doxorubicin-glucuronide prodrug DOX-GA3 for tumour-selective chemotherapy: distribution and efficacy in experimental human ovarian cancer PHJ Houba, E Boven, IH Van der Meulen-Muileman, RGG Leenders, ... British journal of cancer 84 (4), 550-557, 2001 | 99 | 2001 |
Characterization of novel anthracycline prodrugs activated by human β-glucuronidase for use in antibody-directed enzyme prodrug therapy PHJ Houba, RGG Leenders, E Boven, JW Scheeren, HM Pinedo, ... Biochemical pharmacology 52 (3), 455-463, 1996 | 93 | 1996 |
Novel anthracycline-spacer-β-glucuronide,-β-glucoside, and-β-galactoside prodrugs for application in selective chemotherapy RGG Leenders, EWP Damen, EJA Bijsterveld, HW Scheeren, PHJ Houba, ... Bioorganic & medicinal chemistry 7 (8), 1597-1610, 1999 | 91 | 1999 |
Synthesis and biological activity of β-glucuronyl carbamate-based prodrugs of paclitaxel as potential candidates for ADEPT DBA de Bont, RGG Leenders, HJ Haisma, I van Der Meulen-Muileman, ... Bioorganic & Medicinal Chemistry 5 (2), 405-414, 1997 | 79 | 1997 |
Pronounced antitumor efficacy of doxorubicin when given as the prodrug DOX‐GA3 in combination with a monoclonal antibody β‐glucuronidase conjugate PHJ Houba, E Boven, IH Van Der Meulen‐Muileman, RGG Leenders, ... International journal of cancer 91 (4), 550-554, 2001 | 68 | 2001 |
β-Glucuronyl carbamate based pro-moieties designed for prodrugs in ADEPT RGG Leenders, KAA Gerrits, R Ruijtenbeek, HW Scheeren, HJ Haisma, ... Tetrahedron Letters 36 (10), 1701-1704, 1995 | 51 | 1995 |
The efficacy of the anthracycline prodrug daunorubicin-GA3 in human ovarian cancer xenografts PHJ Houba, E Boven, CAM Erkelens, RGG Leenders, JW Scheeren, ... British journal of cancer 78 (12), 1600-1606, 1998 | 38 | 1998 |
Synthesis and evaluation of novel daunomycin-phosphate-sulfate-β-glucuronide and-β-glucoside prodrugs for application in ADEPT RGG Leenders, HW Scheeren, PHJ Houba, E Boven, HJ Haisma Bioorganic & Medicinal Chemistry Letters 5 (24), 2975-2980, 1995 | 35 | 1995 |
Anthracycline prodrugs, method for preparation as well as their use in selective chemotherapy RGG Leenders, EWP Damen, JW Scheeren, HJ Haisma, PHJ Houba, ... US Patent 5,710,135, 1998 | 34 | 1998 |
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 | 31 | 2020 |
Distribution and pharmacokinetics of the prodrug daunorubicin-GA3 in nude mice bearing human ovarian cancer xenografts PHJ Houba, E Boven, IH Van der Meulen-Muileman, RGG Leenders, ... Biochemical pharmacology 57 (6), 673-680, 1999 | 26 | 1999 |
HIV replication inhibitors MJ Kukla, DW Ludovici, RW Kavash, BLD De Corte, J Heeres, ... US Patent 7,276,510, 2007 | 25 | 2007 |
Highly diastereoselective synthesis of anomeric beta-O-glycopyranosyl carbamates from isocyanates RGG Leenders, R Ruytenbeek, EWP Damen, HW Scheeren Georg thieme verlag, 1996 | 22 | 1996 |
Paclitaxel prodrugs, method for preparation as well as their use in selective chemotherapy HBA de Bont, RGG Leenders, JW Scheeren, HJ Haisma, D De Vos US Patent 5,760,072, 1998 | 20 | 1998 |
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 | 17 | 2021 |
Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2, 6-dimethylphenyl] amino]-2-2pyrimidinyl] amino] benzonitrile DPR Schils, JJM Willems, BPAMJ Medaer, ETJ Pasquier, PAJ Janssen, ... US Patent 7,399,856, 2008 | 17 | 2008 |
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 |
HIV inhibiting 1, 2, 4-triazines PJ Lewi, PAJ Janssen, MR De Jonge, LMH Koymans, HM Vinkers, ... US Patent 7,585,861, 2009 | 12 | 2009 |
A novel β-d-glycosyl carbamate forming reaction RGG Leenders, HW Scheeren Tetrahedron Letters 41 (47), 9173-9175, 2000 | 11 | 2000 |
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 | 6 | 2022 |