Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Darren Stead"'
Autor:
Jude N. Arokianathar, Will C. Hartley, Calum McLaughlin, Mark D. Greenhalgh, Darren Stead, Sean Ng, Alexandra M. Z. Slawin, Andrew D. Smith
Publikováno v:
Molecules, Vol 26, Iss 21, p 6333 (2021)
The isothiourea-catalyzed enantioselective 1,6-conjugate addition of para-nitrophenyl esters to 2,6-disubstituted para-quinone methides is reported. para-Nitrophenoxide, generated in situ from initial N-acylation of the isothiourea by the para-nitrop
Externí odkaz:
https://doaj.org/article/355f0306f6ad4c5f949bcd0c0470370b
Autor:
James S. Scott, Darren Stead, Bernard Barlaam, Jason Breed, Rodrigo J. Carbajo, Elisabetta Chiarparin, Natalie Cureton, Paul R. J. Davey, David I. Fisher, Eric T. Gangl, Tyler Grebe, Ryan D. Greenwood, Sudhir Hande, Holia Hatoum-Mokdad, Samantha J. Hughes, Thomas A. Hunt, Tony Johnson, Stefan L. Kavanagh, Teresa C. M. Klinowska, Carrie J. B. Larner, Mandy Lawson, Andrew S. Lister, David Longmire, Stacey Marden, Thomas M. McGuire, Caroline McMillan, Lindsay McMurray, Christopher J. Morrow, J. Willem M. Nissink, Thomas A. Moss, Daniel H. O’Donovan, Radoslaw Polanski, Stephen Stokes, Kumar Thakur, Dawn Trueman, Caroline Truman, Michael J. Tucker, Haixia Wang, Nicky Whalley, Dedong Wu, Ye Wu, Bin Yang, Wenzhan Yang
Publikováno v:
Journal of Medicinal Chemistry. 66:2918-2945
Autor:
Tieguang Yao, Liangwei Wu, Craig S. Donald, Douglas Ferguson, Lei Wang, Andrew Pike, Jianyan Wang, Justin Cidado, Dedong Wu, Kurt Gordon Pike, Kumar Thakur, Chungang Gu, Calum Cook, James Horstick, Tyler Grebe, Theresa Proia, Darren Stead, Alexander Hird, Michelle Lamb, Wenlin Shao, Nichole O'Connell, Yun Jiang, Sudhir M. Hande, Bin Yang, Janet Hawkins, Barlaam Bernard Christophe, Neil Sumner, Melissa Vasbinder, Andrew D. Ferguson, Jane E. Moore, Jeffrey G. Varnes, Bryan Roberts, Maryann San Martin, Lisa Drew, Ujjal Sarkar, Allan Dishington, Chris De Savi, Robert Casella, Steve C. Glossop, Jane L. Holmes, Thomas M. McGuire
Publikováno v:
Journal of Medicinal Chemistry. 63:15564-15590
A CDK9 inhibitor having short target engagement would enable a reduction of Mcl-1 activity, resulting in apoptosis in cancer cells dependent on Mcl-1 for survival. We report the optimization of a series of amidopyridines (from compound 2), focusing o
Publikováno v:
Kinsella, A G, Tibbetts, J D, Stead, D & Cresswell, A J 2022, ' N-tosylhydrazones as acceptors for nucleophilic alkyl radicals in photoredox catalysis : A short case study on possible side reactions ', Synthetic Communications, vol. 52, no. 3, pp. 413-423 . https://doi.org/10.1080/00397911.2022.2028844
We report the attempted development of a photoredox-catalyzed α-C–H alkylation reaction of aliphatic amine derivatives, using N-tosylhydrazones as radical alkylating partners. The original intention was to intercept α-aminoalkyl radical intermedi
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ec46aa3f250cc2fe46c84c98d36a911c
Autor:
Lei Wang, Allan Dishington, Jane E. Moore, Kurt Gordon Pike, Wenlin Shao, Andrew Lister, Anil Patel, Lorraine A. Hassall, Sudhir M. Hande, Jane L. Holmes, Douglas Ferguson, Thomas M. McGuire, Jeffrey G. Varnes, Lin Xue, Chungang Gu, Tieguang Yao, Barlaam Bernard Christophe, Lisa Drew, Janet Hawkins, Liangwei Wu, Chris De Savi, Melissa Vasbinder, Andrew D. Ferguson, Darren Stead, Ujjal Sarkar, Michelle Lamb, Nichole O'Connell, Bin Yang, Alexander Hird
Publikováno v:
Journal of medicinal chemistry. 64(20)
Optimization of a series of azabenzimidazoles identified from screening hit 2 and the information gained from a co-crystal structure of the azabenzimidazole-based lead 6 bound to CDK9 led to the discovery of azaindoles as highly potent and selective
Autor:
Haixia Wang, Stefan Kavanagh, Radoslaw Polanski, Eric Gangl, Michael J. Tucker, Jason Breed, Thomas Anthony Hunt, Paul R. J. Davey, Mandy Lawson, Darren Stead, Oona Delpuech, Ye Wu, J. Willem M. Nissink, Barlaam Bernard Christophe, Dedong Wu, Sudhir M. Hande, Amber Balazs, Dermot F. McGinnity, Wenzhan Yang, Thomas A. Moss, Bin Yang, Sladjana Gagrica, Kumar Thakur, Stacey Marden, Tyler Grebe, Daniel Hillebrand O'donovan, Teresa Klinowska, Samantha Jayne Hughes, Kara Herlihy, David I Fisher, Stephen Stokes, Holia Hatoum-Mokdad, Tony Johnson, James S. Scott, Elisabetta Chiarparin, Bo Peng, Sophie L. M. Janbon, Scott Throner, Ryan Greenwood, David Matthew Wilson, Andrew Lister, Stephen Fawell, Hoan Huynh, Jeffrey G. Varnes, Christopher J. Morrow, Rodrigo J. Carbajo
Publikováno v:
Journal of medicinal chemistry. 63(23)
Herein we report the optimization of a series of tricyclic indazoles as selective estrogen receptor degraders (SERD) and antagonists for the treatment of ER+ breast cancer. Structure based design together with systematic investigation of each region
Autor:
Darren Stead, Michael J. Tucker, Steve Stokes, Martin J. Packer, Christopher Hardy, Ross Overman, Scott Boyd, Stuart E. Pearson, Deepa Bhavsar, Andrew D. Campbell, Derek Ogg, Michael Grondine, Sylvie Guichard, Evan Barry, Marianne Schimpl, James M. Smith, Yang Ye, Kristin Goldberg, Thomas Anthony Hunt, Aaron Smith, Crystal Brown, Jason Grant Kettle, Wenlin Shao, Olga Moleva, Rana Anjum, Xiuwei Li, Rhys D.O. Jones
Publikováno v:
Journal of Medicinal Chemistry. 61:8797-8810
While the treatment of gastrointestinal stromal tumors (GISTs) has been revolutionized by the application of targeted tyrosine kinase inhibitors capable of inhibiting KIT-driven proliferation, diverse mutations to this kinase drive resistance to esta
Autor:
Darren Stead, Calum McLaughlin, Jude N. Arokianathar, Will C. Hartley, Alexandra M. Z. Slawin, Sean Ng, Andrew D. Smith, Mark D. Greenhalgh
Publikováno v:
Molecules
Volume 26
Issue 21
Molecules, Vol 26, Iss 6333, p 6333 (2021)
Volume 26
Issue 21
Molecules, Vol 26, Iss 6333, p 6333 (2021)
Funding: We thank the ERC under the European Union's Seventh Framework Programme (FP7/2007-2013)/E.R.C. grant agreement n° 279850, AstraZeneca and EPSRC [EP/M506631/1 (J.N.A.)], Syngenta and the EPSRC Centre for Doctoral Training in Critical Resourc
Publikováno v:
Chemistry - A European Journal. 23:8810-8813
The highly enantioselective alkylation of α-CF3 enolates, generated from triketopiperazines, has been accomplished through use of a bifunctional thiourea organocatalyst to facilitate 1,4-addition to varied enone acceptors. On treatment with appropri
Publikováno v:
Chemical communications (Cambridge, England). 55(29)
Organocatalysed asymmetric Michael additions of substituted triketopiperazines to enones afford products in high yield and enantiomeric ratio (er). Further modification delivers products possessing natural product (NP) scaffolds including diazabicycl