Fast Iterative Synthetic Approach toward Identification of Novel Highly Selective p38 MAP Kinase Inhibitors

Autor: Michael Forster, Rob Winkel, Gerhard Müller, Martin Schröder, Mark Kudolo, Stefan Knapp, Roberta Tesch, Koen F. W. Hekking, Sandra Röhm, Jorg J C Benningshof, Stefan Laufer, Apirat Chaikuad, Benedict-Tilman Berger

Publikováno v: Journal of Medicinal Chemistry. 62:10757-10782

p38 mitogen-activated protein kinases are key mediators of environmental stress response and are promising targets for treatment of inflammatory diseases and cancer. Numerous efforts have led to the discovery of several potent inhibitors; however, so

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c4e9fe381091f0b7d5974be2f00840e
https://doi.org/10.1021/acs.jmedchem.9b01227

Discovery of 2,4-1

Autor: Johan J N, Veerman, Yorik B, Bruseker, Eddy, Damen, Erik H, Heijne, Wendy, van Bruggen, Koen F W, Hekking, Rob, Winkel, Christopher D, Hupp, Anthony D, Keefe, Julie, Liu, Heather A, Thomson, Ying, Zhang, John W, Cuozzo, Andrew J, McRiner, Mark J, Mulvihill, Peter, van Rijnsbergen, Birgit, Zech, Louis M, Renzetti, Lee, Babiss, Gerhard, Müller

Publikováno v: ACS Med Chem Lett

[Image: see text] Herein we report the discovery of 2,4-1H-imidazole carboxamides as novel, biochemically potent, and kinome selective inhibitors of transforming growth factor β-activated kinase 1 (TAK1). The target was subjected to a DNA-encoded ch

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid________::12d9ec47ec0b7cafcb9e7a681001f5ae
https://pubmed.ncbi.nlm.nih.gov/33859795

Synthesis of versatile building blocks through asymmetric hydrogenation of functionalized itaconic acid mono-esters

Autor: Hans E. Schoemaker, Floris P. J. T. Rutjes, Johannes G. de Vries, André H.M. de Vries, Laurent Lefort, Floris L. van Delft, Koen F. W. Hekking

Publikováno v: Advanced Synthesis & Catalysis, 350(1), 85-94. WILEY-V C H VERLAG GMBH
Advanced Synthesis & Catalysis, 350, 1, pp. 85-94
Advanced Synthesis & Catalysis, 350, 85-94

The rhodium-catalyzed asymmetric hydrogenation of several β-substituted itaconic acid mono-esters, using a library of monodentate phosphoramidite and phosphite ligands is described. Two β-alkyl-substituted substrates were readily hydrogenated by th

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ba9805b41b01591412ccddee3af29a0d
https://doi.org/10.1002/adsc.200700307

Effects of Extended Aryl-Substituted Bisoxazoline Ligands in Asymmetric Synthesis - Efficient Synthesis and Application of 4,4′-Bis(1-Naphthyl)-, 4,4′-Bis(2-Naphthyl)- and 4,4′-Bis(9-Anthryl)-2,2′-isopropylidenebis(1,3-oxazolines)

Autor: Floris P. J. T. Rutjes, Jan J. M. Smits, Patrycja Ruskowska, Koen F. W. Hekking, Jadwiga Frelek, Hester L. van Lingen, Floris L. van Delft, Roy P. M. Storcken, Anouk Klaassen

Publikováno v: European Journal of Organic Chemistry. 2005:4975-4987

The steric influence of extended aryl substituents on 2,2′-bis(1,3-oxazoline) ligands was investigated in a series of asymmetric catalytic reactions such as Mukaiyama aldol and Michael reactions, hetero-Diels–Alder processes, and allylic alkylati

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::50760b19663db4a5b908dfa2011f40e1
https://doi.org/10.1002/ejoc.200500566

Cobalt Chloride Complexes of N 3 and N 4 Donor Ligands

Autor: Jan M. M. Smits, Koen F. W. Hekking, Bas de Bruin, Peter H. M. Budzelaar, T. Martijn Kooistra, René de Gelder, Quinten Knijnenburg, Anton W. Gal

Publikováno v: European Journal of Inorganic Chemistry. 2003:648-655

A number of cobalt(II) chloride complexes of pyridine/amine N3 and N4 donors have been prepared and structurally characterised. Even though they are paramagnetic, assignment of the 1H NMR signals was possible in several cases. With the exception of t

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b40b04df77aa4a258014fc140b3b3a90
https://doi.org/10.1002/ejic.200390090