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المؤلفون: Schenkel LB; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Olivieri PR; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Boezio AA; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Deak HL; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Emkey R; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Graceffa RF; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Gunaydin H; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Guzman-Perez A; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Lee JH; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Teffera Y; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Wang W; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Youngblood BD; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Yu VL; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Zhang M; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Gavva NR; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Lehto SG; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States., Geuns-Meyer S; Departments of Medicinal Chemistry, ‡Lead Discovery, §Molecular Structure, and ∥Pharmacokinetics and Drug Metabolism, Amgen, Inc. , 360 Binney Street, Cambridge, Massachusetts 02142, United States.; Neuroscience, Amgen, Inc. , One Amgen Center Drive, Thousand Oaks, California 91320, United States.

المصدر: Journal of medicinal chemistry [J Med Chem] 2016 Mar 24; Vol. 59 (6), pp. 2794-809. Date of Electronic Publication: 2016 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: Nerve Tissue Proteins/*antagonists & inhibitors , Oxadiazoles/*chemical synthesis , Oxadiazoles/*pharmacology , Purines/*chemical synthesis , Purines/*pharmacology , Quinazolines/*chemical synthesis , Quinazolines/*pharmacology , Transient Receptor Potential Channels/*antagonists & inhibitors, Animals ; Biological Transport, Active ; CHO Cells ; Calcium Channels ; Cricetulus ; Dogs ; Dose-Response Relationship, Drug ; Drug Discovery ; High-Throughput Screening Assays ; Humans ; In Vitro Techniques ; Madin Darby Canine Kidney Cells ; Microsomes, Liver/drug effects ; Microsomes, Liver/metabolism ; Models, Molecular ; Pain Measurement/drug effects ; Rats ; Structure-Activity Relationship ; TRPA1 Cation Channel

المؤلفون: Geuns-Meyer S; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Cee VJ; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Deak HL; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Du B; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Hodous BL; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Nguyen HN; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Olivieri PR; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Schenkel LB; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Vaida KR; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Andrews P; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Bak A; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Be X; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Beltran PJ; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Bush TL; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Chaves MK; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Chung G; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Dai Y; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Eden P; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Hanestad K; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Huang L; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Lin MH; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Tang J; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Ziegler B; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Radinsky R; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Kendall R; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Patel VF; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States., Payton M; †Departments of Medicinal Chemistry, ‡Pharmaceutical Research and Development, §Pharmacokinetics and Drug Metabolism, ∥Molecular Structure, and ⊥Oncology Research, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts 02142, United States, and Amgen Inc., One Amgen Center Drive, Thousand Oaks, California 91320, United States.

المصدر: Journal of medicinal chemistry [J Med Chem] 2015 Jul 09; Vol. 58 (13), pp. 5189-207. Date of Electronic Publication: 2015 May 31.

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: Drug Discovery*, Aurora Kinases/*antagonists & inhibitors , Drug Resistance, Multiple/*drug effects , Drug Resistance, Neoplasm/*drug effects , Neoplasms/*drug therapy , Phthalazines/*pharmacology , Protein Kinase Inhibitors/*pharmacology, Animals ; Cell Proliferation/drug effects ; Female ; Humans ; Mice ; Mice, Nude ; Molecular Structure ; Neoplasms/enzymology ; Neoplasms/pathology ; Rats ; Tumor Cells, Cultured ; Xenograft Model Antitumor Assays

المؤلفون: Nguyen HN; Department of Chemistry Research and Discovery, Amgen Inc., 360 Binney St., Cambridge, Massachusetts 02142, USA. hanhn@amgen.com, Cee VJ, Deak HL, Du B, Faber KP, Gunaydin H, Hodous BL, Hollis SL, Krolikowski PH, Olivieri PR, Patel VF, Romero K, Schenkel LB, Geuns-Meyer SD

المصدر: The Journal of organic chemistry [J Org Chem] 2012 Apr 20; Vol. 77 (8), pp. 3887-906. Date of Electronic Publication: 2012 Apr 05.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: American Chemical Society Country of Publication: United States NLM ID: 2985193R Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1520-6904 (Electronic) Linking ISSN: 00223263 NLM ISO Abbreviation: J Org Chem Subsets: MEDLINE

مواضيع طبية MeSH: Benzoates/*chemical synthesis , Benzoates/*chemistry , Hydrazines/*chemical synthesis , Hydrazines/*chemistry , Isoindoles/*chemical synthesis , Isoindoles/*chemistry , Phthalazines/*chemical synthesis , Phthalazines/*chemistry , Phthalimides/*chemistry , Pyrazoles/*chemical synthesis , Pyrazoles/*chemistry, Catalysis ; Halogenation ; Molecular Structure ; Stereoisomerism

المؤلفون: Schenkel LB; Department of Medicinal Chemistry, Amgen, Inc., 360 Binney Street, Cambridge, Massachusetts 02142, USA. laurie.schenkel@amgen.com, Huang X, Cheng A, Deak HL, Doherty E, Emkey R, Gu Y, Gunaydin H, Kim JL, Lee J, Loberg R, Olivieri P, Pistillo J, Tang J, Wan Q, Wang HL, Wang SW, Wells MC, Wu B, Yu V, Liu L, Geuns-Meyer S

المصدر: Journal of medicinal chemistry [J Med Chem] 2011 Dec 22; Vol. 54 (24), pp. 8440-50. Date of Electronic Publication: 2011 Nov 16.

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: Janus Kinase 2/*antagonists & inhibitors , Protein Kinase Inhibitors/*chemical synthesis , Thienopyridines/*chemical synthesis, Animals ; Cell Line, Tumor ; Cell Membrane Permeability ; Crystallography, X-Ray ; Humans ; Janus Kinase 1/chemistry ; Janus Kinase 2/chemistry ; Leukocytes, Mononuclear/drug effects ; Models, Molecular ; Protein Kinase Inhibitors/chemistry ; Protein Kinase Inhibitors/pharmacology ; Protein Structure, Tertiary ; Structure-Activity Relationship ; Swine ; Thienopyridines/chemistry ; Thienopyridines/pharmacology

المؤلفون: Payton M; Department of Oncology Research, Amgen Inc., Thousand Oaks, California 91320, USA. mpayton@amgen.com, Bush TL, Chung G, Ziegler B, Eden P, McElroy P, Ross S, Cee VJ, Deak HL, Hodous BL, Nguyen HN, Olivieri PR, Romero K, Schenkel LB, Bak A, Stanton M, Dussault I, Patel VF, Geuns-Meyer S, Radinsky R, Kendall RL

المصدر: Cancer research [Cancer Res] 2010 Dec 01; Vol. 70 (23), pp. 9846-54. Date of Electronic Publication: 2010 Oct 08.

نوع المنشور: Journal Article

بيانات الدورية: Publisher: American Association for Cancer Research Country of Publication: United States NLM ID: 2984705R Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1538-7445 (Electronic) Linking ISSN: 00085472 NLM ISO Abbreviation: Cancer Res Subsets: MEDLINE

مواضيع طبية MeSH: Drug Resistance, Neoplasm/*drug effects , Neoplasms/*drug therapy , Phthalazines/*pharmacology , Protein Kinase Inhibitors/*pharmacology , Protein Serine-Threonine Kinases/*antagonists & inhibitors, Adult ; Animals ; Aurora Kinase A ; Aurora Kinase B ; Aurora Kinases ; Benzamides/pharmacology ; Cell Line, Tumor ; Cell Proliferation/drug effects ; Clinical Trials as Topic ; Dose-Response Relationship, Drug ; Drug Evaluation, Preclinical ; Female ; HCT116 Cells ; HeLa Cells ; Histones/metabolism ; Humans ; Mice ; Mice, Nude ; Mutation ; Neoplasms/enzymology ; Neoplasms/pathology ; Organophosphates/pharmacology ; Paclitaxel/pharmacology ; Phosphorylation/drug effects ; Piperazines/pharmacology ; Protein Serine-Threonine Kinases/genetics ; Protein Serine-Threonine Kinases/metabolism ; Pyrazoles/pharmacology ; Quinazolines/pharmacology ; Xenograft Model Antitumor Assays