Publications by authors named "Keith Menear"

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1
1-substituted (Dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-ones endowed with dual DNA-PK/PI3-K inhibitory activity.
Céline Cano, Kappusamy Saravanan, Chris Bailey, Julia Bardos, Nicola J Curtin, Keith A Menear

J Med Chem· August 2013

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Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: the discovery of AZD8055 and AZD2014.
Kurt G Pike, Karine Malagu, Marc G Hummersone, Keith A Menear, Heather M E Duggan

Bioorg Med Chem Lett· March 2013

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Chemosensitization of cancer cells by KU-0060648, a dual inhibitor of DNA-PK and PI-3K.
Joanne M Munck, Michael A Batey, Yan Zhao, Helen Jenkins, Caroline J Richardson, Keith Menear

Mol Cancer Ther· August 2012

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DNA-dependent protein kinase (DNA-PK) inhibitors: structure-activity relationships for O-alkoxyphenylchromen-4-one probes of the ATP-binding domain.
Kate M Clapham, Julia Bardos, M Raymond V Finlay, Bernard T Golding, Edward J Griffen, Keith A Menear

Bioorg Med Chem Lett· February 2011

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DNA-dependent protein kinase (DNA-PK) inhibitors. Synthesis and biological activity of quinolin-4-one and pyridopyrimidin-4-one surrogates for the chromen-4-one chemotype.
Céline Cano, Olivier R Barbeau, Christine Bailey, Xiao-Ling Cockcroft, Nicola J Curtin, Keith A Menear

J Med Chem· December 2010

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AZD8055 is a potent, selective, and orally bioavailable ATP-competitive mammalian target of rapamycin kinase inhibitor with in vitro and in vivo antitumor activity.
Christine M Chresta, Barry R Davies, Ian Hickson, Tom Harding, Sabina Cosulich, Keith Menear

Cancer Res· January 2010

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Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR.
Keith A Menear, Sylvie Gomez, Karine Malagu, Christine Bailey, Kristel Blackburn

Bioorg Med Chem Lett· October 2009

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The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase.
Karine Malagu, Heather Duggan, Keith Menear, Marc Hummersone, Sylvie Gomez

Bioorg Med Chem Lett· October 2009

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Improved ATM kinase inhibitor KU-60019 radiosensitizes glioma cells, compromises insulin, AKT and ERK prosurvival signaling, and inhibits migration and invasion.
Sarah E Golding, Elizabeth Rosenberg, Nicholas Valerie, Isa Hussaini, Mark Frigerio, Keith A Menear

Mol Cancer Ther· October 2009

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The P1N-isopropyl motif bearing hydroxyethylene dipeptide isostere analogues of aliskiren are in vitro potent inhibitors of the human aspartyl protease renin.
Yasuchika Yamaguchi, Keith Menear, Nissim-Claude Cohen, Robert Mah, Frédéric Cumin

Bioorg Med Chem Lett· August 2009

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4-[3-(4-cyclopropanecarbonylpiperazine-1-carbonyl)-4-fluorobenzyl]-2H-phthalazin-1-one: a novel bioavailable inhibitor of poly(ADP-ribose) polymerase-1.
Keith A Menear, Claire Adcock, Robert Boulter, Xiao-ling Cockcroft, Louise Copsey

J Med Chem· October 2008

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8-Biarylchromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK).
Marine Desage-El Murr, Celine Cano, Bernard T Golding, Ian R Hardcastle, Marc Hummersome, Keith Menear

Bioorg Med Chem Lett· September 2008

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Novel alkoxybenzamide inhibitors of poly(ADP-ribose) polymerase.
Keith A Menear, Claire Adcock, Francisco Cuenca Alonso, Kristel Blackburn, Louise Copsey

Bioorg Med Chem Lett· July 2008

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Pyranone, thiopyranone, and pyridone inhibitors of phosphatidylinositol 3-kinase related kinases. Structure-activity relationships for DNA-dependent protein kinase inhibition, and identification of the first potent and selective inhibitor of the ataxia telangiectasia mutated kinase.
Jonathan J Hollick, Laurent J M Rigoreau, Celine Cano-Soumillac, Xiaoling Cockcroft, Nicola J Curtin, Keith A Menear

J Med Chem· April 2007

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Phthalazinones 2: Optimisation and synthesis of novel potent inhibitors of poly(ADP-ribose)polymerase.
Xiao-Ling Cockcroft, Krystyna J Dillon, Lesley Dixon, Jan Drzewiecki, Frank Kerrigan, Keith A Menear

Bioorg Med Chem Lett· February 2006

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Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase.
Vincent M Loh, Xiao-ling Cockcroft, Krystyna J Dillon, Lesley Dixon, Jan Drzewiecki, Keith A Menear

Bioorg Med Chem Lett· May 2005

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