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المؤلفون: Zhao Y; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Mahy W; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Willis NJ; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Woodward HL; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Steadman D; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Bayle ED; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Atkinson BN; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Sipthorp J; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Vecchia L; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Ruza RR; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Harlos K; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Jeganathan F; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Constantinou S; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Costa A; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Kjær S; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Bictash M; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Salinas PC; Department of Cell and Developmental Biology, Laboratory for Molecular and Cellular Biology, University College London, London WC1E 6BT, U.K., Whiting P; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K., Vincent JP; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Fish PV; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, The Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Jones EY; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K.

المصدر: ACS chemical neuroscience [ACS Chem Neurosci] 2022 Jul 06; Vol. 13 (13), pp. 2060-2077. Date of Electronic Publication: 2022 Jun 22.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 101525337 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1948-7193 (Electronic) Linking ISSN: 19487193 NLM ISO Abbreviation: ACS Chem Neurosci Subsets: MEDLINE

مواضيع طبية MeSH: Crystallography, X-Ray*

المؤلفون: Willis NJ; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Mahy W; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Sipthorp J; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Zhao Y; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Woodward HL; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Atkinson BN; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Bayle ED; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Svensson F; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Frew S; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Jeganathan F; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Monaghan A; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Benvegnù S; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Jolly S; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Vecchia L; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Ruza RR; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Kjær S; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Howell S; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Snijders AP; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Bictash M; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Salinas PC; Department of Cell and Developmental Biology, Laboratory for Molecular and Cellular Biology, University College London, London WC1E 6BT, U.K., Vincent JP; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Jones EY; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Whiting P; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Fish PV; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2022 May 26; Vol. 65 (10), pp. 7212-7230. Date of Electronic Publication: 2022 May 10.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

مواضيع طبية MeSH: Enzyme Inhibitors*/chemistry , Enzyme Inhibitors*/pharmacology , Esterases*/metabolism, Brain/metabolism ; Crystallography, X-Ray ; Wnt Signaling Pathway

المؤلفون: Bayle ED; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Svensson F; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Atkinson BN; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Steadman D; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Willis NJ; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Woodward HL; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Whiting P; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Vincent JP; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Fish PV; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2021 Apr 22; Vol. 64 (8), pp. 4289-4311. Date of Electronic Publication: 2021 Mar 30.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

مواضيع طبية MeSH: Wnt Signaling Pathway*/drug effects, Enzyme Inhibitors/*chemistry , Esterases/*antagonists & inhibitors, Binding Sites ; Catalytic Domain ; Cell Nucleus/metabolism ; Cytoplasm/metabolism ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacology ; Esterases/metabolism ; Humans ; Molecular Dynamics Simulation ; Small Molecule Libraries/chemistry ; Small Molecule Libraries/metabolism ; Small Molecule Libraries/pharmacology

المؤلفون: Mahy W; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Willis NJ; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Zhao Y; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Woodward HL; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Svensson F; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Sipthorp J; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Vecchia L; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Ruza RR; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Hillier J; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Kjær S; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Frew S; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Monaghan A; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Bictash M; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Salinas PC; Department of Cell and Developmental Biology, Laboratory for Molecular and Cellular Biology, University College London, London WC1E 6BT, U.K., Whiting P; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K., Vincent JP; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K., Jones EY; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, U.K., Fish PV; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, U.K.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2020 Nov 12; Vol. 63 (21), pp. 12942-12956. Date of Electronic Publication: 2020 Oct 30.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

مواضيع طبية MeSH: Enzyme Inhibitors/*chemistry , Esterases/*antagonists & inhibitors , Oxadiazoles/*chemistry, Administration, Oral ; Animals ; Binding Sites ; Blood-Brain Barrier/drug effects ; Blood-Brain Barrier/metabolism ; Crystallography, X-Ray ; Drug Design ; Enzyme Inhibitors/pharmacokinetics ; Enzyme Inhibitors/pharmacology ; Esterases/metabolism ; Half-Life ; Humans ; Inhibitory Concentration 50 ; Male ; Mice ; Mice, Inbred C57BL ; Microsomes, Liver/metabolism ; Molecular Dynamics Simulation ; Oxadiazoles/pharmacokinetics ; Oxadiazoles/pharmacology ; Structure-Activity Relationship ; Wnt Signaling Pathway/drug effects

المؤلفون: Mahy W; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom., Patel M; Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, United Kingdom., Steadman D; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom., Woodward HL; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom., Atkinson BN; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom., Svensson F; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, United Kingdom., Willis NJ; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom., Flint A; Department of Chemistry, University College London, 20 Gordon Street, London WC1H 0AJ, United Kingdom., Papatheodorou D; UCL School of Pharmacy, University College London, 29-39 Brunswick Square, Bloomsbury, London WC1N 1AX, United Kingdom., Zhao Y; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, United Kingdom., Vecchia L; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, United Kingdom., Ruza RR; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, United Kingdom., Hillier J; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, United Kingdom., Frew S; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom., Monaghan A; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom., Costa A; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom., Bictash M; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom., Walter MW; Eli Lilly, Erl Wood Manor, Windlesham, Surrey GU20 6PH, United Kingdom., Jones EY; Division of Structural Biology, Wellcome Centre for Human Genetics, University of Oxford, The Henry Wellcome Building for Genomic Medicine, Roosevelt Drive, Oxford OX3 7BN, United Kingdom., Fish PV; Alzheimer's Research UK UCL Drug Discovery Institute, University College London, Cruciform Building, Gower Street, London WC1E 6BT, United Kingdom.; The Francis Crick Institute, 1 Midland Road, Kings Cross, London NW1 1AT, United Kingdom.

المصدر: Journal of medicinal chemistry [J Med Chem] 2020 Sep 10; Vol. 63 (17), pp. 9464-9483. Date of Electronic Publication: 2020 Aug 18.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

مواضيع طبية MeSH: Carboxylic Ester Hydrolases/*antagonists & inhibitors , Enzyme Inhibitors/*chemistry , Enzyme Inhibitors/*pharmacology , Pyrroles/*chemistry , Pyrroles/*pharmacology , Pyrrolidines/*chemistry , Pyrrolidines/*pharmacology, Carboxylic Ester Hydrolases/chemistry ; Drug Evaluation, Preclinical ; Models, Molecular ; Protein Conformation

المؤلفون: Bellenie BR, Cheung KJ, Varela A, Pierrat OA, Collie GW, Box GM, Bright MD, Gowan S, Hayes A, Rodrigues MJ, Shetty KN, Carter M, Davis OA, Henley AT, Innocenti P, Johnson LD, Liu M, de Klerk S, Le Bihan YV, Lloyd MG, McAndrew PC, Shehu E, Talbot R, Woodward HL, Burke R, Kirkin V, van Montfort RLM, Raynaud FI, Rossanese OW, Hoelder S

المصدر: Journal of medicinal chemistry [J Med Chem] 2020 Apr 23; Vol. 63 (8), pp. 4047-4068. Date of Electronic Publication: 2020 Apr 10.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

مواضيع طبية MeSH: Benzimidazoles/*administration & dosage , Benzimidazoles/*chemistry , Drug Delivery Systems/*methods , Drug Discovery/*methods , Proto-Oncogene Proteins c-bcl-6/*antagonists & inhibitors , Proto-Oncogene Proteins c-bcl-6/*metabolism, Animals ; Cell Line, Tumor ; Female ; Humans ; Male ; Mice ; Mice, Inbred BALB C ; Mice, SCID ; Microsomes, Liver/drug effects ; Microsomes, Liver/metabolism ; Protein Structure, Tertiary ; Rats ; Rats, Sprague-Dawley ; Xenograft Model Antitumor Assays/methods

المؤلفون: Anderhub SJ; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Mak GW; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Gurden MD; The Breast Cancer Toby Robins Research Centre, The Institute of Cancer Research, London, United Kingdom., Faisal A; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Drosopoulos K; The Breast Cancer Toby Robins Research Centre, The Institute of Cancer Research, London, United Kingdom., Walsh K; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Woodward HL; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Innocenti P; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Westwood IM; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Naud S; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Hayes A; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Theofani E; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Filosto S; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Saville H; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Burke R; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., van Montfort RLM; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Raynaud FI; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Blagg J; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Hoelder S; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Eccles SA; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom., Linardopoulos S; Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, The Institute of Cancer Research, London, United Kingdom. spiros.linardopoulos@icr.ac.uk.; The Breast Cancer Toby Robins Research Centre, The Institute of Cancer Research, London, United Kingdom.

المصدر: Molecular cancer therapeutics [Mol Cancer Ther] 2019 Oct; Vol. 18 (10), pp. 1696-1707.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Association for Cancer Research, Inc Country of Publication: United States NLM ID: 101132535 Publication Model: Print Cited Medium: Internet ISSN: 1538-8514 (Electronic) Linking ISSN: 15357163 NLM ISO Abbreviation: Mol Cancer Ther Subsets: MEDLINE

مواضيع طبية MeSH: Cell Cycle Checkpoints*/drug effects, Pyrimidines/*pharmacology , Spindle Apparatus/*metabolism , Triazoles/*pharmacology , Triple Negative Breast Neoplasms/*pathology, Animals ; Biological Availability ; Cell Cycle/drug effects ; Cell Cycle Proteins/antagonists & inhibitors ; Cell Cycle Proteins/metabolism ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Chromosome Segregation/drug effects ; Chromosomes, Human/genetics ; Drug Synergism ; Humans ; Mice ; PTEN Phosphohydrolase/metabolism ; Paclitaxel/pharmacology ; Paclitaxel/therapeutic use ; Protein Serine-Threonine Kinases/antagonists & inhibitors ; Protein Serine-Threonine Kinases/metabolism ; Protein-Tyrosine Kinases/antagonists & inhibitors ; Protein-Tyrosine Kinases/metabolism ; Pyrimidines/chemistry ; Spindle Apparatus/drug effects ; Triazoles/chemistry ; Triple Negative Breast Neoplasms/drug therapy

المؤلفون: Woodward HL; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Innocenti P; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Cheung KJ; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Hayes A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Roberts J; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Henley AT; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Faisal A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Mak GW; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Box G; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Westwood IM; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.; Division of Structural Biology , The Institute of Cancer Research , London SW3 6JB , United Kingdom., Cronin N; Division of Structural Biology , The Institute of Cancer Research , London SW3 6JB , United Kingdom., Carter M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Valenti M; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., De Haven Brandon A; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., O'Fee L; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Saville H; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Schmitt J; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Burke R; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Broccatelli F; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., van Montfort RLM; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.; Division of Structural Biology , The Institute of Cancer Research , London SW3 6JB , United Kingdom., Raynaud FI; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Eccles SA; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Linardopoulos S; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.; The Breakthrough Breast Cancer Research Centre, Division of Breast Cancer Research , The Institute of Cancer Research , London SW3 6JB , United Kingdom., Blagg J; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom., Hoelder S; Cancer Research UK Cancer Therapeutics Unit at The Institute of Cancer Research , London SM2 5NG , United Kingdom.

المصدر: Journal of medicinal chemistry [J Med Chem] 2018 Sep 27; Vol. 61 (18), pp. 8226-8240. Date of Electronic Publication: 2018 Sep 10.

نوع المنشور: Journal Article; Research Support, Non-U.S. Gov't

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 9716531 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-4804 (Electronic) Linking ISSN: 00222623 NLM ISO Abbreviation: J Med Chem Subsets: MEDLINE

مواضيع طبية MeSH: Drug Discovery*, Cell Cycle Proteins/*antagonists & inhibitors , Microsomes, Liver/*metabolism , Protein Kinase Inhibitors/*chemistry , Protein Kinase Inhibitors/*pharmacology , Protein Serine-Threonine Kinases/*antagonists & inhibitors , Protein-Tyrosine Kinases/*antagonists & inhibitors , Pyrimidines/*chemistry , Pyrimidines/*pharmacology , Triazoles/*chemistry , Triazoles/*pharmacology, Animals ; Cell Cycle Proteins/metabolism ; Cells, Cultured ; Clinical Trials, Phase I as Topic ; Female ; Humans ; Male ; Methylation ; Mice ; Microsomes, Liver/drug effects ; Models, Molecular ; Molecular Structure ; Protein Conformation ; Protein Kinase Inhibitors/pharmacokinetics ; Protein Serine-Threonine Kinases/metabolism ; Protein-Tyrosine Kinases/metabolism ; Pyrimidines/pharmacokinetics ; Rats ; Rats, Sprague-Dawley ; Structure-Activity Relationship ; Tissue Distribution ; Triazoles/pharmacokinetics

المؤلفون: Atkinson BN; Alzheimer's Research UK UCL Drug Discovery Institute, The Cruciform Building, University College London, Gower Street, London, WC1E 6BT, UK. p.fish@ucl.ac.uk., Woodward HL; Alzheimer's Research UK UCL Drug Discovery Institute, The Cruciform Building, University College London, Gower Street, London, WC1E 6BT, UK. p.fish@ucl.ac.uk., Sipthorp J; Alzheimer's Research UK UCL Drug Discovery Institute, The Cruciform Building, University College London, Gower Street, London, WC1E 6BT, UK. p.fish@ucl.ac.uk., Fish PV; Alzheimer's Research UK UCL Drug Discovery Institute, The Cruciform Building, University College London, Gower Street, London, WC1E 6BT, UK. p.fish@ucl.ac.uk.

المصدر: Organic & biomolecular chemistry [Org Biomol Chem] 2017 Nov 29; Vol. 15 (46), pp. 9794-9799.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Royal Society of Chemistry Country of Publication: England NLM ID: 101154995 Publication Model: Print Cited Medium: Internet ISSN: 1477-0539 (Electronic) Linking ISSN: 14770520 NLM ISO Abbreviation: Org Biomol Chem Subsets: MEDLINE

مواضيع طبية MeSH: Epoxy Compounds/*chemistry , Heat-Shock Proteins/*chemistry , Hydroxylamines/*chemical synthesis, Animals ; Hydroxylamines/chemistry ; Male ; Mice ; Molecular Structure ; Stereoisomerism