Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Mario van Zeeland"'
Autor:
Hortense Deronzier, Cecile Dorleans, John Waller, Laurent Saniere, Andre Fouquet, Fiona Elizabeth Andrews, Mark Baugh, J.C.M. Uitdehaag, George McGarry, Phil Jones, Ann Mitchell, Emma Kinghorn, Eric Nicolai, Wilson Caulfield, Zoran Rankovic, Dominique Potin, Mario van Zeeland, Wullie Arbuckle, Jennifer Kerr, Jiaqiang Cai, Mark Wheaton Anderson, Iain Martin, Maureen Dempster, Ashvin Mistry, François Chevallier, William Finlay, Clive Long, Robinson John E, Xavier Fradera, Paul Westwood, Iain Cumming
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:6237-6241
Several structure-guided optimisation strategies were explored in order to improve the hERG selectivity profile of cathepsin K inhibitor 1 , whilst maintaining its otherwise excellent in vitro and in vivo profile. Ultimately, attenuation of c log P a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::dbcfb747e700da9944dc50d293047fcc
https://doi.org/10.1016/j.bmcl.2010.08.101
https://doi.org/10.1016/j.bmcl.2010.08.101
Autor:
D. Jonathan Bennett, Kenneth S. Cameron, John Bruin, Mario van Zeeland, Xavier Fradera, J.C.M. Uitdehaag, Emma Kinghorn, Jiaqiang Cai, Maureen Dempster, Paul Westwood, Lucy Popplestone, Mark Baugh, Robinson John E, William Hamilton, Clive Long
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4507-4510
Using computer aided modelling studies, a new extended P2/S2 interaction was identified. This extended region can accommodate a variety of functional groups, such as aryls and basic amines. It was discovered that the N3 nitrogen of the pyrimidine-2-c
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b6a4ef389f50e29987f14e5b21317077
https://doi.org/10.1016/j.bmcl.2010.06.043
https://doi.org/10.1016/j.bmcl.2010.06.043
Autor:
T.M. Meulemans, Jonathan Gillespie, D. Jonathan Bennett, Darcey Black, Ann Mitchell, Kenneth S. Cameron, J.C.M. Uitdehaag, Maurice Maidment, Mario van Zeeland, Fiona Elizabeth Andrews, Sylviane Boucharens, Allard Kaptein, Maureen Dempster, Emma Kinghorn, Mark Baugh, Jiaqiang Cai, Philip Jones, Zoran Rankovic, Paul Westwood, Martijn Bastiani, Iain Martin, Iain Cumming, Leon van Berkom, Paul Vink, Paul Scullion, Xavier Fradera, John Bruin, Robinson John E, William Hamilton, Clive Long
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:4350-4354
6-Phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile analogues were identified as potent and selective cathepsin S inhibitor against both purified enzyme and in human JY cell based cellular assays. This core has a very stable thio-trapping nitrile war-h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::78adb9c4a5619dc58c16a256a3eb3516
https://doi.org/10.1016/j.bmcl.2010.06.072
https://doi.org/10.1016/j.bmcl.2010.06.072
Autor:
Eric Nicolai, Clive Long, Ann Mitchell, Maureen Dempster, William Hamilton, Jennifer Kerr, Cecile Dorleans, Iain Martin, Paul Scullion, Hortense Deronzier, John Bruin, Emma Hamilton, Zoran Rankovic, Andre Fouquet, John Robinson, John Waller, Laurent Saniere, Mark Baugh, Fiona Andrews, Jiaqiang Cai, Joost C.M. Uitdehaag, Wilson Caulfield, Dominique Potin, Ashvin Mistry, François Chevallier, Paul Westwood, Emma Kinghorn, George McGarry, Iain Cumming, Mario van Zeeland, X. Fradera
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1524-1527
Morphing structural features of HTS-derived chemotypes led to the discovery of novel 2-cyano-pyrimidine inhibitors of cathepsin K with good pharmacokinetic profiles, for example, compound 20 showed high catK potency (IC(50)=4nM), >580-fold selectivit
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c3024221a3f1580ea5f971d2c310f2b7
https://doi.org/10.1016/j.bmcl.2010.01.100
https://doi.org/10.1016/j.bmcl.2010.01.100
Autor:
Judith Versteegh, Joeri Johannes Petrus De Wit, Arthur Oubrie, Niels Hoogenboom, Tjeerd Barf, Maaike van Hoek, Bert Kazemier, Allard Kaptein, Carsten Schultz-Fademrecht, Paula Leandro-Garcia, Frank Wijnands, John Dulos, Martin Jaeger, Bas van de Kar, Jeroen A.D.M. de Roos, Gerard Mt Vogel, Mario van Zeeland, Edwin de Zwart, Vera de Kimpe, Judith Borsboom
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(12)
The identification of a potent, selective, and orally available MK2 inhibitor series is described. The initial absence of oral bioavailability was successfully tackled by moving the basic nitrogen of the spiro-4-piperidyl moiety towards the electron-
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::69f22fbd250c5e4013286b26a2ff642b
https://pubmed.ncbi.nlm.nih.gov/21565498
https://pubmed.ncbi.nlm.nih.gov/21565498
Autor:
Judith Versteegh, Nicole Seegers, Henri Klop, Tjeerd Barf, Claudia Hofstra, Jeroen A.D.M. de Roos, Carsten Schultz-Fademrecht, Mario van Zeeland, Arthur Oubrie, Bert Kazemier, Maaike van Hoek, Dennis Demont, Allard Kaptein, Jorrit J. Hornberg, Sander de Wilde, Ruben L. Smeets, Bas van de Kar, Ruud van der Heijden, Richard van Someren
Publikováno v:
Bioorganic & Medicinal Chemistry Letters, 21, 3818-22
Bioorganic & Medicinal Chemistry Letters, 21, 12, pp. 3818-22
Bioorganic & Medicinal Chemistry Letters, 21, 12, pp. 3818-22
Item does not contain fulltext MK2 kinase is a promising drug discovery target for the treatment of inflammatory diseases. Here, we describe the discovery of novel MK2 inhibitors using X-ray crystallography and structure-based drug design. The lead h
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1bdeec28829a3848ff7f20ab076a3584
http://hdl.handle.net/2066/97376
http://hdl.handle.net/2066/97376
Autor:
Peter van Rijnsbergen, Kathryn Everett, Simone Belshaw, D. Jonathan Bennett, Wullie Arbuckle, Maureen Dempster, Emma Kinghorn, Xavier Fradera, Mark Baugh, Jiaqiang Cai, Zoran Rankovic, Paul Westwood, John Bruin, William Hamilton, Clive Long, T.M. Meulemans, Philip Jones, Mario van Zeeland, Jennifer Kerr, J.C.M. Uitdehaag, Lucy Popplestone, Leon van Berkom, Iain Martin, Robinson John E
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(23)
The trifluoromethylphenyl P2 motif from previously reported heteroarylnitrile series has been successfully applied for the design and synthesis of highly potent novel ketoamide-based cathepsin S inhibitors. The key in this process is the change of th
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b3a43d1f132eeef39158411039e24986
https://pubmed.ncbi.nlm.nih.gov/21030256
https://pubmed.ncbi.nlm.nih.gov/21030256
Autor:
Iain Cumming, Andre Fouquet, Hortense Deronzier, Mark Baugh, William Finlay, Emma Kinghorn, Zoran Rankovic, Jiaqiang Cai, Eric Nicolai, Maureen Dempster, Mario van Zeeland, François Chevallier, Jennifer Kerr, Sylviane Boucharens, George McGarry, William Hamilton, Xavier Fradera, J.C.M. Uitdehaag, Robinson John E, Laurent Saniere, Dominique Potin, Jonathan Gillespie, John Bruin, Paul Scullion, D. Jonathan Bennett, Cecile Dorleans, Kenneth S. Cameron
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(15)
Starting from previously disclosed equally potent cathepsin K and S inhibitor 4-propyl-6-(3-trifluoromethylphenyl)pyrimidine-2-carbonitrile 1, a novel 2-phenyl-9H-purine-6-carbonitrile scaffold was identified to provide potent and selective cathepsin
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e98bd55a43ebd81843ae171f54be9d64
https://pubmed.ncbi.nlm.nih.gov/20594841
https://pubmed.ncbi.nlm.nih.gov/20594841
Autor:
Sylviane Boucharens, Joost C.M. Uitdehaag, Jonathan Gillespie, Mario van Zeeland, Zoran Rankovic, Jiaqiang Cai, Maureen Dempster, Clive Long, Iain Cumming, Ann Mitchell, Emma Hamilton, Ashvin Mistry, Craig Jamieson, Angela King, X. Fradera
Publikováno v:
Bioorganicmedicinal chemistry letters. 20(5)
A novel dioxo-triazine series of cathepsin K inhibitors was identified from HTS. A rapid exploratory programme led to the discovery of potent and selective cathepsin K inhibitors, typified by compound 24 which displayed IC(50) values of 17nM against
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53fdab9708c58710341cb4f40df927f7
https://pubmed.ncbi.nlm.nih.gov/20153187
https://pubmed.ncbi.nlm.nih.gov/20153187