Zobrazeno 1 - 10
of 57
pro vyhledávání: '"Eva M, Lenz"'
Autor:
Iain A. Cumming, Sébastien L. Degorce, Anna Aagaard, Erin L. Braybrooke, Nichola L. Davies, Coura R. Diène, Andrew J. Eatherton, Hannah R. Felstead, Sam D. Groombridge, Eva M. Lenz, Yunxia Li, Youfeng Nai, Stuart Pearson, Graeme R. Robb, James S. Scott, Oliver R. Steward, Chengyan Wu, Yafeng Xue, Lanping Zhang, Yanxiu Zhang
Publikováno v:
Bioorganicmedicinal chemistry. 63
In this article, we report the discovery of a series of pyrimidopyridones as inhibitors of IRAK4 kinase. From a previously disclosed 5-azaquinazoline series, we found that switching the pyridine ring for an N-substituted pyridone gave a novel hinge b
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::24a392e9908e5c3f41f7d9cc5004c347
https://pubmed.ncbi.nlm.nih.gov/35439688
https://pubmed.ncbi.nlm.nih.gov/35439688
Autor:
Darren Cross, Matthew J. Martin, Carine M. Guérot, Nicolas Floc'h, Clare Gregson, Jonathan P. Orme, Michal Bista, Lin Xue, Xu Li, Amar Rahi, Xiliang Zhao, Richard A. Ward, L. Evans, Gail L. Wrigley, Arash Mosallanejad, Tieguang Yao, Claire McWhirter, David J. Hargreaves, Nicola Colclough, Sue Bickerton, Darren Mckerrecher, Peter Barton, Yang Ye, Yi Liu, Marta Wylot, M. Raymond V. Finlay, Xiaoming Kang, Eva M. Lenz, Daniel O'Neill, Verity Talbot, Olivier Lorthioir, Paul D. Smith
Publikováno v:
Journal of medicinal chemistry. 64(18)
The epidermal growth factor receptor (EGFR) harboring activating mutations is a clinically validated target in non-small-cell lung cancer, and a number of inhibitors of the EGFR tyrosine kinase domain, including osimertinib, have been approved for cl
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::58199c545ee296c2c44cec7db12bfba5
https://pubmed.ncbi.nlm.nih.gov/34491761
https://pubmed.ncbi.nlm.nih.gov/34491761
Autor:
Jennifer H. Pink, James S. Scott, Nicola Lindsay, Alan Rosen, Andrew Bloecher, Yafeng Xue, Lisa Drew, Sébastien L. Degorce, Graeme R. Robb, Christopher Thomas Halsall, Rana Anjum, Eva M. Lenz, Rodrigo J. Carbajo, Keith Dillman, Michele Mayo
Publikováno v:
Journal of Medicinal Chemistry. 62:9918-9930
In this article, we report the discovery of a series of 5-azaquinazolines as selective IRAK4 inhibitors. From modestly potent quinazoline 4, we introduced a 5-aza substitution to mask the 4-NH hydrogen bond donor (HBD). This allowed us to substitute
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::9fd9bcc98a875ec7b6d96417a1d726e0
https://doi.org/10.1021/acs.jmedchem.9b01346
https://doi.org/10.1021/acs.jmedchem.9b01346
Autor:
Richard Lonsdale, Richard A. Ward, Nicola Colclough, Eva M. Lenz, Jonathan Burgess, Nichola L. Davies, Alexandra L. Orton
Publikováno v:
Journal of Chemical Information and Modeling. 57:3124-3137
Targeted covalent inhibition is an established approach for increasing the potency and selectivity of potential drug candidates, as well as identifying potent and selective tool compounds for target validation studies. It is evident that identificati
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d9ae23b627f759d44b4f07520d214eb8
https://doi.org/10.1021/acs.jcim.7b00553
https://doi.org/10.1021/acs.jcim.7b00553
Autor:
Sébastien L, Degorce, Rana, Anjum, Andrew, Bloecher, Rodrigo J, Carbajo, Keith S, Dillman, Lisa, Drew, Christopher T, Halsall, Eva M, Lenz, Nicola A, Lindsay, Michele F, Mayo, Jennifer H, Pink, Graeme R, Robb, Alan, Rosen, James S, Scott, Yafeng, Xue
Publikováno v:
Journal of medicinal chemistry. 62(21)
In this article, we report the discovery of a series of 5-azaquinazolines as selective IRAK4 inhibitors. From modestly potent quinazoline
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::8929c269d95a7fdb4b89ef21869d21c5
https://pubmed.ncbi.nlm.nih.gov/31622099
https://pubmed.ncbi.nlm.nih.gov/31622099
Autor:
David G. Temesi, Malcolm R. Clench, Alexandra L. Orton, Eva M. Lenz, Scott W. Martin, Robin Smith
Publikováno v:
Rapid Communications in Mass Spectrometry. 31:145-151
Rationale: The incubation of CPAQOP (1-[(2R)-2-[[4-[3-chloro-4-(2-pyridyloxy)anilino]quinazolin-5-yl]oxymethyl]-1-piperidyl]-2-hydroxy) with human liver microsomes generated several metabolites that highlighted the hydroxyacetamide side chain was a m
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::0e570af1a2d28abf3a7710a7f1261bd1
https://doi.org/10.1002/rcm.7772
https://doi.org/10.1002/rcm.7772
Autor:
Sébastien L. Degorce, Franck Lach, Eva M. Lenz, Catherine B. Trigwell, Sarah L. Pass, Martin Pass, Clifford David Jones, Richard Ducray, Christopher Thomas Halsall, Scott Boyd, Jon Curwen
Publikováno v:
Journal of Medicinal Chemistry. 59:4859-4866
Optimization of cellular lipophilic ligand efficiency (LLE) in a series of 2-anilino-pyrimidine IGF-1R kinase inhibitors led to the identification of novel 2-(pyrazol-4-ylamino)-pyrimidines with improved physicochemical properties. Replacement of the
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9efaf5ebeeae34b71f735e8482dcb57c
https://doi.org/10.1021/acs.jmedchem.6b00203
https://doi.org/10.1021/acs.jmedchem.6b00203
Autor:
Yafeng Xue, Lisa Drew, Rana Anjum, Sébastien L. Degorce, Keith Dillman, James S. Scott, Christopher Thomas Halsall, Sam D. Groombridge, Stephen Stokes, Jennifer H. Pink, Eva M. Lenz, Nicola Lindsay, Michele Mayo, Graeme R. Robb
Publikováno v:
Bioorganicmedicinal chemistry. 26(4)
We have developed a series of orally efficacious IRAK4 inhibitors, based on a scaffold hopping strategy and using rational structure based design. Efforts to tackle low permeability and high efflux in our previously reported pyrrolopyrimidine series
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b96a864f63d65def4ea1c7ab68158308
https://pubmed.ncbi.nlm.nih.gov/29398441
https://pubmed.ncbi.nlm.nih.gov/29398441
Autor:
Matteo Zanda, Nick Bushby, Michael J. Hickey, Eva M. Lenz, Andrea Testa, Monica Piras, Charles S. Elmore, Ian N. Fleming
Publikováno v:
Synlett. 25:1019-1025
Tritiated compounds are invaluable tools for in vitro and in vivo studies on bioactive molecules. Here we describe a ‘click-chemistry’-based strategy for deuteration and tritiation of multifunctional compounds and multimodal molecular imaging pro
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c4755aca73d4975a5d6cd7e225858936
https://doi.org/10.1055/s-0033-1340940
https://doi.org/10.1055/s-0033-1340940
Autor:
Scott, Martin, Eva M, Lenz, Robin, Smith, David G, Temesi, Alexandra L, Orton, Malcolm R, Clench
Publikováno v:
Rapid communications in mass spectrometry : RCM. 31(1)
The incubation of CPAQOP (1-[(2R)-2-[[4-[3-chloro-4-(2-pyridyloxy)anilino]quinazolin-5-yl]oxymethyl]-1-piperidyl]-2-hydroxy) with human liver microsomes generated several metabolites that highlighted the hydroxyacetamide side chain was a major site o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=pmid________::ced9d7c4486a7079d3eed865e5ba9496
https://pubmed.ncbi.nlm.nih.gov/27943491
https://pubmed.ncbi.nlm.nih.gov/27943491