Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Ruben Gerardus George Leenders"'
Autor:
Eddy Damen, Albert Galera-Prat, Piotr Nieczypor, Jo Waaler, Sudarshan Murthy, Sven T. Sowa, Sjoerd Aertssen, Ruben Gerardus George Leenders, Max Lycke, Marc Nazaré, Shoshy Alam Brinch, Stefan Krauss, Lari Lehtiö, Anita Wegert
Publikováno v:
Journal of Medicinal Chemistry
Tankyrases 1 and 2 are central biotargets in the WNT/β-catenin signaling and Hippo signaling pathways. We have previously developed tankyrase inhibitors bearing a 1,2,4-triazole moiety and binding predominantly to the adenosine binding site of the t
Autor:
Christoph Schächtele, Jan E. Ehlert, Ruben Gerardus George Leenders, Daniel Müller, Daniel Feger, Danny C. Lenstra, Jasmin Mecinović, Federica Trivarelli, Remco Zijlmans, Gerhard Müller, Bart van Bree, Anita Wegert, Marc van de Sande, Eddy Damen, Carolin Heidemann-Dinger, Michael H.G. Kubbutat
Publikováno v:
Bioorganic & Medicinal Chemistry Letters, 29, 2516-2524
Bioorganic & Medicinal Chemistry Letters, 29, 17, pp. 2516-2524
Bioorganic & Medicinal Chemistry Letters, 29, 17, pp. 2516-2524
Detailed structure activity relationship of two series of quinazoline EHMT1/EHMT2 inhibitors (UNC0224 and UNC0638) have been elaborated. New and active alternatives are presented for the ubiquitous substitution patterns found in literature for the li
Publikováno v:
Tetrahedron Letters. 61:151369
A novel reaction giving easy access to 5-bromopyrimidines via the cyclization of 1,2-dibromoenones and amidines is described.
Autor:
Danny C. Lenstra, Ruben Gerardus George Leenders, Jasmin Mecinović, Richard H. Blaauw, Anita Wegert, Eddy Damen, Floris P. J. T. Rutjes
Publikováno v:
Chemmedchem, 13, 14, pp. 1405-1413
Chemmedchem, 13, 1405-1413
Chemmedchem, 13, 1405-1413
SETD7 is a histone H3K4 lysine methyltransferase involved in human gene regulation. Aberrant expression of SETD7 has been associated with various diseases, including cancer. Therefore, SETD7 is considered a good target for the development of new epig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ad6207eb960f60220fdb327ae3daa2c
https://doi.org/10.1002/cmdc.201800242
https://doi.org/10.1002/cmdc.201800242
Autor:
Johan Wilhelm Scheeren, I.H. van der Meulen-Muileman, Epie Boven, Ruben Gerardus George Leenders, P. H. J. Houba, Hidde J. Haisma, Herbert M. Pinedo
Publikováno v:
British Journal of Cancer
British Jounal of Cancer, 84(4), 550-557. Nature Publishing Group
British Jounal of Cancer, 84(4), 550-557. Nature Publishing Group
The doxorubicin (DOX) prodrug N-[4-doxorubicin-N-carbonyl (oxymethyl) phenyl] O-beta -glucuronyl carbamate (DOX-GA3) was synthesised for specific activation by human beta -glucuronidase, which is released in necrotic areas of tumour lesions. This nov
Autor:
Vandenput Dirk Alfons Leo, Remco Zijlmans, Paul J. Lewi, Jan Heeres, Ruben Gerardus George Leenders, Jerome Emile Georges Guillemont
Publikováno v:
European Journal of Organic Chemistry. 2010:2852-2854
An optimized procedure is given for the synthesis of novel 3-(arylamino)-1,2,4-triazin-5-one building blocks from commercially available material. By employing these building blocks, a practical protocol is described for the functionalization of the
Autor:
H.M. Pinedo, I.H. van der Meulen-Muileman, Epie Boven, Johan Wilhelm Scheeren, Hidde J. Haisma, P. H. J. Houba, Ruben Gerardus George Leenders
Publikováno v:
University of Groningen
N-[4-daunorubicin-N-carbonyl (oxymethyl)phenyl] O-beta-glucuronyl carbamate (DNR-GA3) is a glucuronide prodrug of daunorubicin (DNR) which induced a better tumor growth delay than DNR when studied at equitoxic doses in three human ovarian cancer xeno
Autor:
Hans W. Scheeren, Ida H van der Meulen-Muileman, Ruben Gerardus George Leenders, Hidde J. Haisma, Dries B.A. de Bont
Publikováno v:
de Bont, D B A, Leenders, R G G, Haisma, H J, van der Meulen-Muileman, I & Scheeren, H W 1997, ' Synthesis and biological activity of ß-glucuronyl-carbamate-based prodrugs of paclitaxel as potential candidates in ADEPT ', Bioorganic and Medicinal Chemistry, vol. 5, pp. 405-414 . https://doi.org/10.1016/S0968-0896(96)00249-0
Bioorganic and Medicinal Chemistry, 5, 405-414. Elsevier Limited
Bioorganic and Medicinal Chemistry, 5, 405-414. Elsevier Limited
The syntheses of prodrugs of paclitaxel, which can be used in ADEPT in order to target paclitaxel towards tumor cells, are described. The prodrugs 1 and 2a,b consist of a spacer molecule connected via a carbamate linkage to a beta-glucuronic acid. Th
Publikováno v:
Synthesis. 1996:1309-1312
Autor:
Johannes W Scheeren, P. H. J. Houba, Ruben Gerardus George Leenders, Herbert M. Pinedo, Hidde J. Haisma, Epie Boven
Publikováno v:
University of Groningen
Antibody-directed enzyme prodrug therapy (ADEPT) aims at the specific activation of a prodrug by an enzyme-immunoconjugate localized in tumor tissue. The use of an enzyme of human origin is preferable in ADEPT because it might not be immunogenic when