Výsledky vyhledávání - "Xiao-Ling Fan Cockcroft"

Identification and optimisation of novel and selective small molecular weight kinase inhibitors of mTOR

Autor: Sylvie Gomez, Karine Malagu, Thomas Presnot, Sally Ewen, Mihiro Sunose, Xiao-Ling Fan Cockcroft, Niall M. B. Martin, Alexandra Fundo, Armelle Le Gall, Keith Allan Menear, Hermann Gesine Johanna, Luisa Sebastian, Kristel Blackburn, Ian Hickson, Christine Bailey, Graeme C. M. Smith, Eleanor Torode, Kurt Gordon Pike

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:5898-5901

A pharmacophore mapping approach, derived from previous experience of PIKK family enzymes, was used to identify a hit series of selective inhibitors of the mammalian target of rapamycin (mTOR). Subsequent refinement of the SAR around this hit series

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5847355afd0c1842bfbfbdcbcce2b812
https://doi.org/10.1016/j.bmcl.2009.08.069

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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

Autor: Kristoffer Valerie, Laurent Rigoreau, Nicholas C.K. Valerie, Marc Geoffrey Hummersone, Isa M. Hussaini, Keith Allan Menear, Lawrence F. Povirk, Wei Yee Chong, Mark Frigerio, Elizabeth Rosenberg, Xiao-Ling Fan Cockcroft, Mark J. O'Connor, Timothy E. Van Meter, Sarah E. Golding

Publikováno v: Molecular Cancer Therapeutics. 8:2894-2902

Ataxia telangiectasia (A-T) mutated (ATM) is critical for cell cycle checkpoints and DNA repair. Thus, specific small molecule inhibitors targeting ATM could perhaps be developed into efficient radiosensitizers. Recently, a specific inhibitor of the

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1968cb23965407def87e6ccde7eb291
https://doi.org/10.1158/1535-7163.mct-09-0519

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Studies on Pyrrolopyrimidines as Selective Inhibitors of Multidrug-Resistance- Associated Protein in Multidrug Resistance

Autor: Warren Miller, Simon Cocks, Deanne Thompson, Sukhjit Sohal, Prakash Mistry, John Milton, Richard Faint, Stephen Paul Wren, John W. Scott, Irina Chuckowree, Shouming Wang, Lyndsay Smith, Xiao-Ling Fan Cockcroft, Paul Depledge, Hazel Jones, Nigel Vicker, Adrian Folkes

Publikováno v: Journal of Medicinal Chemistry. 47:1329-1338

Multidrug resistance mediated by P-glycoprotein (Pgp) or multidrug-resistance-associated protein (MRP) remains a major obstacle for successful treatment of cancer. Inhibition of Pgp and MRP transport is important for high efficacy of anticancer drugs

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7724a058846c53792538d116bb44cc93
https://doi.org/10.1021/jm031011g

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[Untitled]

Autor: Xiao Ling Fan Cockcroft, Mark C. Allen, Markus Gruetter, John P. Priestle

Publikováno v: Journal of Computer-Aided Molecular Design. 13:579-588

This paper describes the construction, validation and application of an active site model of the serine protease thrombin. Initial use was made of medium resolution X-ray crystallographic structures of thrombin complexed with low molecular weight, no

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::a1131beed94c52cb32147b30aae683fd
https://doi.org/10.1023/a:1008098615891

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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

Autor: Xiao-Ling Fan Cockcroft, Graeme C. M. Smith, Marc Geoffrey Hummersone, David R. Newell, Mark Frigerio, Heather Mary Ellen Duggan, Olivier Barbeau, Christine Bailey, Nicola J. Curtin, Bernard T. Golding, Ian R. Hardcastle, Caroline Richardson, Charlotte Knights, Roger J. Griffin, Ben Spittle, Celine Cano, Keith Allan Menear

Publikováno v: Journal of medicinal chemistry. 53(24)

Following the discovery of dibenzo[b,d]thiophen-4-yl)-2-morpholino-4H-chromen-4-one (NU7441) ( Leahy , J. J. J. ; Golding , B. T. ; Griffin , R. J. ; Hardcastle , I. R. ; Richardson , C. ; Rigoreau , L. ; Smith , G. C. M. Bioorg. Med. Chem. Lett. 200

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7234ff7d985a1c75601a34997f10fc05
https://pubmed.ncbi.nlm.nih.gov/21080722

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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

Autor: Rachel Ord, Ian Hickson, Mark Frigerio, Niall M. B. Martin, Sophie Guiard, Keith Allan Menear, Marc Geoffrey Hummersone, Celine Cano-Soumillac, Jonathan J Hollick, Xiao-Ling Fan Cockcroft, Roger J. Griffin, Laurent Rigoreau, Graeme C. M. Smith, Bernard T. Golding, Ian R. Hardcastle, Caroline Richardson, David R. Newell, Ian Timothy Williams Matthews, Nicola J. Curtin

Publikováno v: Journal of medicinal chemistry. 50(8)

Structure-activity relationships have been investigated for inhibition of DNA-dependent protein kinase (DNA-PK) and ATM kinase by a series of pyran-2-ones, pyran-4-ones, thiopyran-4-ones, and pyridin-4-ones. A wide range of IC50 values were observed

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::86fd293330798965b03b89cd699d51c3
https://pubmed.ncbi.nlm.nih.gov/17371003

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Phthalazinones 2: Optimization and Synthesis of Novel Potent Inhibitors of Poly(ADP-Ribose)polymerase

Autor: Lesley Dixon, Jan Drzewiecki, Graeme C. M. Smith, Keith Allan Menear, Krystyna J. Dillon, Xiao-Ling Fan Cockcroft, Frank Kerrigan, Niall M. B. Martin, Vincent M. Loh

Publikováno v: ChemInform. 37

We have previously described the discovery of poly(ADP-ribose)polymerase-1 (PARP-1) inhibitors based on a phthalazinone scaffold. Subsequent optimisation of inhibitory activity, metabolic stability and pharmacokinetic parameters has led to a novel se

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2b141432495a1fecbf7ee6b92e1d55a5
https://doi.org/10.1002/chin.200621153

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Discovery of potent chromen-4-one inhibitors of the DNA-dependent protein kinase (DNA-PK) using a small-molecule library approach

Autor: Bernard T. Golding, Nicola J. Curtin, Marine Desage El-Murr, Roger J. Griffin, Martin Stockley, Laurent Rigoreau, Graeme C. M. Smith, Ian R. Hardcastle, Xiao-Ling Fan Cockcroft, Caroline Richardson, Justin J J Leahy

Publikováno v: Journal of medicinal chemistry. 48(24)

Structure-activity relationships for inhibition of DNA-dependent protein kinase (DNA-PK) have been defined for substituted chromen-4-ones. For the 2-amino-substituted benzo[h]chromen-4-ones, a morpholine substituent at this position was essential for

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::706da803d15339b6f42fa26768a912bf
https://pubmed.ncbi.nlm.nih.gov/16302822

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Phthalazinones. Part 1: The design and synthesis of a novel series of potent inhibitors of poly(ADP-ribose)polymerase

Autor: Graeme C. M. Smith, Sylvie Gomez, Alan Whittle, Jane Paul, Xiao-Ling Fan Cockcroft, Roger F. Newton, Penny Jane Eversley, Janet Hoare, Keith Allan Menear, Ian Timothy William Matthews, Frank Kerrigan, Lesley Dixon, Krystyna J. Dillon, Julia Vile, Niall M. B. Martin, Jan Drzewiecki, Vincent M. Loh

Publikováno v: Bioorganicmedicinal chemistry letters. 15(9)

Screening of the Maybridge compound collection identified 4-arylphthalazinones as micromolar inhibitors of PARP-1 catalytic activity. Subsequent optimisation of both inhibitory activity and metabolic stability led to a novel series of meta-substitute

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16ed804bc96146aa9169a550ceac1b90
https://pubmed.ncbi.nlm.nih.gov/15837300

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