Zobrazeno 1 - 10
of 12
pro vyhledávání: '"John Thomas Feutrill"'
Autor:
Thomas W. Gero, John Thomas Feutrill, Bailing Chen, Nathanael S. Gray, Feru Frederic, Brian J. Groendyke, Hilary Szabo, Zhengnian Li, Bin Li, David A. Scott, Chelsea E. Powell
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(19)
The protein kinase TNK2 (ACK1) is an emerging drug target for a variety of indications, in particular for cancer where it plays a key role transmitting cell survival, growth and proliferative signals via modification of multiple downstream effectors
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::220bb5eba35eecf2c507de3c0f2c8533
https://pubmed.ncbi.nlm.nih.gov/32739400
https://pubmed.ncbi.nlm.nih.gov/32739400
Autor:
Alexandra L. Garnham, Peter E. Czabotar, Andrew F. Wilks, Stefan P Glaser, Peter Hall, Scott Taylor, Mark A. Dawson, John Thomas Feutrill, Zhen Xu, Carl R. Walkley, Phillip P. Sharp, Kate E. Jarman, Tamas Hatfaludi, Helene Jousset, David J. Segal, Christopher J. Burns, Jean-Marc Garnier, David C.S. Huang, Dean Tyler, Anthony Nicholas Cuzzupe
Publikováno v:
ACS Medicinal Chemistry Letters. 8:1298-1303
A number of diazepines are known to inhibit bromo- and extra-terminal domain (BET) proteins. Their BET inhibitory activity derives from the fusion of an acetyl-lysine mimetic heterocycle onto the diazepine framework. Herein we describe a straightforw
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f53a8629f367b983d223e262028099ee
https://doi.org/10.1021/acsmedchemlett.7b00389
https://doi.org/10.1021/acsmedchemlett.7b00389
Autor:
Brian J. Groendyke, John Thomas Feutrill, Thomas W. Gero, Zhengnian Li, David A. Scott, Feru Frederic, Chelsea E. Powell, Hilary Szabo, Kevin Pang, Bailing Chen, Bin Li, Nathanael S. Gray
Publikováno v:
Bioorganicmedicinal chemistry letters. 30(4)
The SAR of a series of benzopyrimidodiazepinone inhibitors of TNK2 was developed, starting from the potent and selective compound XMD8-87. A diverse set of anilines was introduced in an effort to improve the in vivo PK profile and minimize the risk o
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::19fad4c04cad6c1f0bdde67bcc8337e5
https://pubmed.ncbi.nlm.nih.gov/31928839
https://pubmed.ncbi.nlm.nih.gov/31928839
Autor:
Gavin Bennett, Anne J. Rüger, John Thomas Feutrill, Rosemary Lynch, Ann Lewis, Anthea L. Newton, Nico Zinn, Tammy Ladduwahetty, Sunose Mihiro, Andrew Cansfield, Giovanna Bergamini, Oliver Rausch, Alan P. Watt, Douglas W. Thomson, Katie Ellard
Publikováno v:
ACS Medicinal Chemistry Letters. 7:768-773
CZ415, a potent ATP-competitive mTOR inhibitor with unprecedented selectivity over any other kinase is described. In addition to a comprehensive characterization of its activities in vitro, in vitro ADME, and in vivo pharmacokinetic data are reported
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3c737c2b53bd2e69fa1983934fa60781
https://doi.org/10.1021/acsmedchemlett.6b00149
https://doi.org/10.1021/acsmedchemlett.6b00149
Autor:
Laura Andrau, Margarita Kurek, R Marcel Kling, Andrew Craig Donohue, Harrison Sikanyika, David M. Shackleford, Andrew F. Wilks, John Thomas Feutrill, Tracy L. Nero, Emmanuelle Fantino, Herbert R. Treutlein, Michelle Farrugia, Ian D Phillips, Michelle Leanne Styles, David Gerard Bourke, Jun Zeng, Thao Kim Nu Nguyen, Christopher J. Burns, James T. Palmer, Max Joffe, Xianyong Bu, Stephen Su, Susan A. Charman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5887-5892
A series of phenylaminopyrimidines has been identified as inhibitors of Janus kinases (JAKs). Development of this initial series led to the potent JAK2/JAK1 inhibitor CYT387 (N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-benzam
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ac0ae62a5d282604aedf6d7be8aa9d41
https://doi.org/10.1016/j.bmcl.2009.08.071
https://doi.org/10.1016/j.bmcl.2009.08.071
Publikováno v:
Tetrahedron. 64:4880-4895
The total syntheses of crocacins A–D are described. The key steps were a syn-aldol reaction followed by anti-reduction to secure the stereotetrad and acylation of an ene- or dienecarbamate to form the enamide.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1c0e6326a0524f1b7682f419ca111368
https://doi.org/10.1016/j.tet.2008.01.139
https://doi.org/10.1016/j.tet.2008.01.139
Autor:
Philippe Chamiot-Clerc, Christelle Mugler, Nathalie Derimay, John Thomas Feutrill, Jacques Le Roux, Frank Halley, Claudine Grepin, Caroline Leriche, David Papin, Laurent Schio
Publikováno v:
Bioorganicmedicinal chemistry letters. 26(2)
A new series of pyrazolo[1,5-a]pyrimidines exemplified by compound 1, has been identified with moderate activity (IC50=165nM), following GSK256066 rescaffolding. Compound 1 optimization at positions 2, 3, 6 and 7 gave compound 10 with high in vitro a
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d74d975afb98aee33bc583f80731c51
https://pubmed.ncbi.nlm.nih.gov/26681511
https://pubmed.ncbi.nlm.nih.gov/26681511
Autor:
Ferdows Hilli, John Thomas Feutrill, Georgina A. Holloway, Helmut M. Hügel, Mark A. Rizzacasa
Publikováno v:
Tetrahedron Letters. 41:8569-8572
Two routes to the unusual 12-membered unsaturated benzolactone of the highly cytotoxic marine metabolites the salicylihalamides are presented. The first involves an RCM step to construct the C9C10 alkene bond and this provided the model macrolacto
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::1b05234933c6433101402e81cd2f8f04
https://doi.org/10.1016/s0040-4039(00)01420-9
https://doi.org/10.1016/s0040-4039(00)01420-9
Publikováno v:
ChemInform. 39
The total syntheses of crocacins A–D are described. The key steps were a syn-aldol reaction followed by anti-reduction to secure the stereotetrad and acylation of an ene- or dienecarbamate to form the enamide.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::6e9a2152c89cbf189d201ac3a8a6e455
https://doi.org/10.1002/chin.200840184
https://doi.org/10.1002/chin.200840184
Publikováno v:
Organic letters. 4(4)
[structure: see text] The first asymmetric synthesis of (+)-crocacin D (4) is described. The key steps in the sequence are the stereoselective assembly of the stereotetrad via a substrate-controlled aldol reaction and anti-selective reduction, format
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::506df116f08895268da21fa82e4e1e89
https://pubmed.ncbi.nlm.nih.gov/11843582
https://pubmed.ncbi.nlm.nih.gov/11843582