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المؤلفون: Humphreys PG; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Atkinson SJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Bamborough P; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Bit RA; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Chung CW; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Craggs PD; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Cutler L; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Davis R; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Ferrie A; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Gong G; WuXi Shanghai STA Pharmaceutical R&D Co., Ltd., No. 90 Delin Road, WaiGaoQiao Free Trade Zone, Shanghai 200131, China., Gordon LJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Gray M; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Harrison LA; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Hayhow TG; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Haynes A; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Henley N; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Hirst DJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Holyer ID; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Lindon MJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Lovatt C; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Lugo D; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., McCleary S; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Molnar J; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Osmani Q; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Patten C; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Preston A; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Rioja I; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Seal JT; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Smithers N; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Sun F; WuXi Shanghai STA Pharmaceutical R&D Co., Ltd., No. 90 Delin Road, WaiGaoQiao Free Trade Zone, Shanghai 200131, China., Tang D; WuXi Shanghai STA Pharmaceutical R&D Co., Ltd., No. 90 Delin Road, WaiGaoQiao Free Trade Zone, Shanghai 200131, China., Taylor S; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Theodoulou NH; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom.; WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde, Thomas Graham Building, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Thomas C; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Watson RJ; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Wellaway CR; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom., Zhu L; WuXi Shanghai STA Pharmaceutical R&D Co., Ltd., No. 90 Delin Road, WaiGaoQiao Free Trade Zone, Shanghai 200131, China., Tomkinson NCO; WestCHEM, Department of Pure and Applied Chemistry, University of Strathclyde, Thomas Graham Building, 295 Cathedral Street, Glasgow G1 1XL, United Kingdom., Prinjha RK; GlaxoSmithKline R&D, Stevenage, Hertfordshire SG1 2NY, United Kingdom.

المصدر: Journal of medicinal chemistry [J Med Chem] 2022 Feb 10; Vol. 65 (3), pp. 2262-2287. Date of Electronic Publication: 2022 Jan 07.

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 Design*, Aminoquinolines/*chemistry , Proteins/*metabolism, Administration, Oral ; Aminoquinolines/metabolism ; Aminoquinolines/pharmacokinetics ; Aminoquinolines/therapeutic use ; Animals ; Benzoates/chemistry ; Benzoates/metabolism ; Binding Sites ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Crystallography, X-Ray ; Dogs ; Half-Life ; Humans ; Male ; Mice ; Molecular Conformation ; Molecular Dynamics Simulation ; Neoplasms/drug therapy ; Proteins/antagonists & inhibitors ; Rats ; Structure-Activity Relationship

المؤلفون: Seal JT, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Foley J; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Gordon L, Grandi P; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstr. 1, 69117 Heidelberg, Germany., Gray JRJ, Harrison LA, Kruger RG; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Matteo JJ; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., McCabe MT; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Taylor S, Wall ID, Watson RJ, Woolven JM, Wyce A; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Zhang XP; Cancer Epigenetics Research Unit, GlaxoSmithKline, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States., Demont EH

المصدر: Journal of medicinal chemistry [J Med Chem] 2021 Aug 12; Vol. 64 (15), pp. 10772-10805. Date of Electronic Publication: 2021 Jul 13.

نوع المنشور: Journal Article

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: Furans/*pharmacology , Proteins/*antagonists & inhibitors , Pyrazoles/*pharmacology, Dose-Response Relationship, Drug ; Furans/chemistry ; Humans ; Molecular Structure ; Proteins/metabolism ; Pyrazoles/chemistry ; Structure-Activity Relationship

المؤلفون: Harrison LA; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Atkinson SJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Bassil A; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Chung CW; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Grandi P; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstr. 1, 69117 Heidelberg, Germany., Gray JRJ; Quantitative Pharmacology, Immunoinflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Levernier E; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Lewis A; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Lugo D; Quantitative Pharmacology, Immunoinflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Messenger C; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Michon AM; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstr. 1, 69117 Heidelberg, Germany., Mitchell DJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Preston A; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Prinjha RK; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Rioja I; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Seal JT; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Taylor S; Quantitative Pharmacology, Immunoinflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Wall ID; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Watson RJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Woolven JM; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Demont EH; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2021 Aug 12; Vol. 64 (15), pp. 10742-10771. Date of Electronic Publication: 2021 Jul 07.

نوع المنشور: Journal Article

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: Cell Cycle Proteins/*antagonists & inhibitors , Pyridines/*pharmacology , Transcription Factors/*antagonists & inhibitors, Cell Cycle Proteins/metabolism ; Dose-Response Relationship, Drug ; Humans ; Models, Molecular ; Molecular Structure ; Pyridines/chemistry ; Structure-Activity Relationship ; Transcription Factors/metabolism

المؤلفون: Aylott HE; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Atkinson SJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Bamborough P; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Bassil A; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Chung CW; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Gordon L; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Grandi P; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstr. 1, Heidelberg 69117, Germany., Gray JRJ; Quantitative Pharmacology, Immunoinflammation Therapy Area Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Harrison LA; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Hayhow TG; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Messenger C; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Mitchell D; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Phillipou A; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Preston A; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Prinjha RK; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Rianjongdee F; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Rioja I; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Seal JT; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Wall ID; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Watson RJ; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Woolven JM; Platform Technology and Science, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K., Demont EH; Epigenetics Discovery Performance Unit, GlaxoSmithKline, Medicines Research Centre, Stevenage, Hertfordshire SG1 2NY, U.K.

المصدر: Journal of medicinal chemistry [J Med Chem] 2021 Mar 25; Vol. 64 (6), pp. 3249-3281. Date of Electronic Publication: 2021 Mar 04.

نوع المنشور: Journal Article

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: Cell Cycle Proteins/*antagonists & inhibitors , Protein Domains/*drug effects , Small Molecule Libraries/*chemistry , Small Molecule Libraries/*pharmacology , Transcription Factors/*antagonists & inhibitors, Cell Cycle Proteins/chemistry ; Cell Cycle Proteins/metabolism ; Drug Design ; Drug Discovery ; Humans ; Transcription Factors/chemistry ; Transcription Factors/metabolism

المؤلفون: Seal JT, Atkinson SJ, Aylott H, Bamborough P, Chung CW, Copley RCB, Gordon L, Grandi P; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Gray JRJ, Harrison LA, Hayhow TG, Lindon M, Messenger C, Michon AM; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Mitchell D, Preston A, Prinjha RK, Rioja I, Taylor S; IVIVT Cellzome, Platform Technology and Science, GlaxoSmithKline, Meyerhofstrasse 1, 69117 Heidelberg, Germany., Wall ID, Watson RJ, Woolven JM, Demont EH

المصدر: Journal of medicinal chemistry [J Med Chem] 2020 Sep 10; Vol. 63 (17), pp. 9093-9126. Date of Electronic Publication: 2020 Aug 30.

نوع المنشور: Journal Article

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: Ligands*, Anti-Inflammatory Agents/*chemistry , Transcription Factors/*antagonists & inhibitors, Administration, Oral ; Amides/chemistry ; Amides/metabolism ; Amides/pharmacokinetics ; Animals ; Anti-Inflammatory Agents/metabolism ; Anti-Inflammatory Agents/pharmacokinetics ; Binding Sites ; Cell Cycle Proteins/antagonists & inhibitors ; Cell Cycle Proteins/metabolism ; Crystallography, X-Ray ; Dogs ; Half-Life ; Humans ; Hydrogen Bonding ; Male ; Molecular Dynamics Simulation ; Protein Domains ; Rats ; Rats, Wistar ; Structure-Activity Relationship ; Transcription Factors/metabolism

المؤلفون: Morse MA; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK. Electronic address: Mary.A.Morse@gsk.com., Balogh KK; The Jake Gittlen Cancer Research Foundation, H069, Department of Pathology, C7800, The Pennsylvania State University, College of Medicine, 500 University Drive, Hershey, PA 17033-0850, USA., Brendle SA; The Jake Gittlen Cancer Research Foundation, H069, Department of Pathology, C7800, The Pennsylvania State University, College of Medicine, 500 University Drive, Hershey, PA 17033-0850, USA., Campbell CA; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Chen MX; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Furze RC; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Harada IL; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Holyer ID; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Kumar U; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Lee K; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Prinjha RK; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Rüdiger M; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Seal JT; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Taylor S; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Witherington J; GlaxoSmithKline Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire, SG1 2NY, UK., Christensen ND; The Jake Gittlen Cancer Research Foundation, H069, Department of Pathology, C7800, The Pennsylvania State University, College of Medicine, 500 University Drive, Hershey, PA 17033-0850, USA.

المصدر: Antiviral research [Antiviral Res] 2018 Jun; Vol. 154, pp. 158-165. Date of Electronic Publication: 2018 Apr 11.

نوع المنشور: Journal Article; Research Support, N.I.H., Extramural

بيانات الدورية: Publisher: Elsevier Country of Publication: Netherlands NLM ID: 8109699 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1872-9096 (Electronic) Linking ISSN: 01663542 NLM ISO Abbreviation: Antiviral Res

مواضيع طبية MeSH: Benzodiazepines/*therapeutic use , Heterocyclic Compounds, 4 or More Rings/*therapeutic use , Nuclear Proteins/*antagonists & inhibitors , Papillomaviridae/*drug effects , Transcription Factors/*antagonists & inhibitors , Warts/*drug therapy, Acetylation ; Animals ; Cell Line, Tumor ; Cell Survival ; Epigenesis, Genetic ; Lysine ; Male ; Papillomaviridae/genetics ; Protein Domains ; Rabbits ; Warts/virology

المؤلفون: Bamborough P; Epinova DPU, Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline R&D, Medicines Research Centre, Gunnels Wood Road, Stevenage, Hertfordshire SG1 2NY, UK. Paul.a.Bamborough@gsk.com, Diallo H, Goodacre JD, Gordon L, Lewis A, Seal JT, Wilson DM, Woodrow MD, Chung CW

المصدر: Journal of medicinal chemistry [J Med Chem] 2012 Jan 26; Vol. 55 (2), pp. 587-96. Date of Electronic Publication: 2012 Jan 11.

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: Anti-Inflammatory Agents, Non-Steroidal/*chemical synthesis , Protein Serine-Threonine Kinases/*antagonists & inhibitors , Sulfonamides/*chemistry, Anti-Inflammatory Agents, Non-Steroidal/chemistry ; Anti-Inflammatory Agents, Non-Steroidal/pharmacology ; Cell Cycle Proteins ; Crystallography, X-Ray ; Cytokines/biosynthesis ; Fluorescence Polarization ; Humans ; Isoxazoles/chemical synthesis ; Isoxazoles/chemistry ; Isoxazoles/pharmacology ; Leukocytes, Mononuclear/drug effects ; Leukocytes, Mononuclear/metabolism ; Models, Molecular ; Molecular Structure ; Nuclear Proteins/chemistry ; Protein Binding ; Protein Serine-Threonine Kinases/chemistry ; Solubility ; Structure-Activity Relationship ; Sulfonamides/chemical synthesis ; Sulfonamides/pharmacology ; Surface Plasmon Resonance ; Transcription Factors/chemistry

المؤلفون: Westaway SM; Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts, SG1 2NY, UK. sue.m.westaway@gsk.com, Brown SL, Fell SC, Johnson CN, MacPherson DT, Mitchell DJ, Myatt JW, Stanway SJ, Seal JT, Stemp G, Thompson M, Lawless K, McKay F, Muir AI, Barford JM, Cluff C, Mahmood SR, Matthews KL, Mohamed S, Smith B, Stevens AJ, Bolton VJ, Jarvie EM, Sanger GJ

المصدر: Journal of medicinal chemistry [J Med Chem] 2009 Feb 26; Vol. 52 (4), pp. 1180-9.

نوع المنشور: Journal Article

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

مواضيع طبية MeSH: Drug Discovery*, Gastrointestinal Agents/*pharmacology , Piperazines/*pharmacology , Piperidines/*pharmacology , Pyloric Antrum/*drug effects , Receptors, Gastrointestinal Hormone/*agonists , Receptors, Neuropeptide/*agonists, Animals ; Dogs ; Gastrointestinal Motility/drug effects ; Humans ; Muscle Contraction/drug effects ; Piperazines/chemistry ; Piperidines/chemistry ; Pyloric Antrum/physiology ; Rabbits ; Rats

المؤلفون: Westaway SM; Immuno-Inflammation Centre of Excellence for Drug Discovery, GlaxoSmithKline, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts SG1 2NY, UK. sue.m.westaway@gsk.com, Brown SL, Conway E, Heightman TD, Johnson CN, Lapsley K, Macdonald GJ, MacPherson DT, Mitchell DJ, Myatt JW, Seal JT, Stanway SJ, Stemp G, Thompson M, Celestini P, Colombo A, Consonni A, Gagliardi S, Riccaboni M, Ronzoni S, Briggs MA, Matthews KL, Stevens AJ, Bolton VJ, Boyfield I, Jarvie EM, Stratton SC, Sanger GJ

المصدر: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Dec 15; Vol. 18 (24), pp. 6429-36. Date of Electronic Publication: 2008 Oct 19.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: Elsevier Science Ltd Country of Publication: England NLM ID: 9107377 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1464-3405 (Electronic) Linking ISSN: 0960894X NLM ISO Abbreviation: Bioorg Med Chem Lett Subsets: MEDLINE

مواضيع طبية MeSH: Carbon/*chemistry , Pyridines/*chemistry , Receptors, Gastrointestinal Hormone/*agonists , Receptors, Neuropeptide/*agonists, Animals ; Chemistry, Pharmaceutical/methods ; Drug Design ; Gastrins/chemistry ; Humans ; Inhibitory Concentration 50 ; Kinetics ; Models, Chemical ; Pyridines/chemical synthesis ; Pyridines/pharmacology ; Rabbits ; Rats ; Receptors, Gastrointestinal Hormone/chemistry ; Receptors, Neuropeptide/chemistry