يعرض 1 - 10 نتائج من 27 نتيجة بحث عن '"Joseph"', وقت الاستعلام: 1.53s تنقيح النتائج
  1. 1
    Targeting Chikungunya Virus Replication by Benzoannulene Inhibitors

    المؤلفون: Mark T. Heise, Thomas E. Morrison, Subramaniam Ananthan, Joseph A. Maddry, Sanjay Sarkar, Jessica L. Smith, Kevin J Rodzinak, Nicole N. Haese, Daniel N. Streblow, Nathaniel J. Moorman, Cassilyn E. Streblow, Ashish K. Pathak, Vibha Pathak, Aaron D Streblow, Lynn Rasmussen, Fahim Ahmad, Corinne E. Augelli-Szafran, S Kaleem Ahmed, Victor R. DeFilippis, Robert Bostwick, Craig N. Kreklywich, Mark J. Suto, Sixue Zhang, Robbie Allen, Alec J. Hirsch, Jaden T Cowan, Babu L. Tekwani, Kiley Bonin, Nichole A. Tower, Wes Sander, Valerie J Smith, Mousheng Wu, John M Gerdes, Clayton R. Morrison, Omar Moukha-Chafiq

    المصدر: J Med Chem

    مصطلحات موضوعية: Male, Oxidoreductases Acting on CH-CH Group Donors, Cell Survival, Dihydroorotate Dehydrogenase, Virus Replication, Antiviral Agents, 01 natural sciences, Article, Virus, Cell Line, Mice, Structure-Activity Relationship, 03 medical and health sciences, chemistry.chemical_compound, In vivo, Drug Discovery, Benzene Derivatives, medicine, Animals, Humans, Benzamide, Cytotoxicity, 030304 developmental biology, 0303 health sciences, Binding Sites, Chemistry, virus diseases, Virology, 0104 chemical sciences, Mice, Inbred C57BL, Molecular Docking Simulation, Disease Models, Animal, 010404 medicinal & biomolecular chemistry, Titer, Mechanism of action, Viral replication, Microsomes, Liver, Dihydroorotate dehydrogenase, Chikungunya Fever, Molecular Medicine, Female, medicine.symptom, Chikungunya virus, Half-Life

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1cd9fc90c3516c776e90ca2779eb4634
    https://doi.org/10.1021/acs.jmedchem.0c02183

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  2. 2
    Discovery and Optimization of 2H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer

    المؤلفون: Hongchao Zheng, Andrew L. McIver, Surendra Karavadhi, Adam Yasgar, William J. Moore, Li Liu, Zhuyin Li, Carleen Klumpp-Thomas, Ajit Jadhav, Natalia J. Martinez, Kyle R. Brimacombe, Mindy I. Davis, Wei Zhao, Daniel J. Urban, Stephen V. Frye, Anton Simeonov, Xiaodong Wang, Samarjit Patnaik, Rajan Pragani, Mark J. Henderson, Weihe Zhang, Melinda G. Hollingshead, Min Shen, Qingyang Liu, Gordon M. Stott, Tobie D. Lee, Sam Michael, Matthew B. Boxer, Jason M. Rohde, Matthew D. Hall, Yuhong Fang, Joseph M. Covey, Dorian M. Cheff

    المصدر: J Med Chem

    مصطلحات موضوعية: IDH1, Pyridines, Pyridones, Mutant, Drug Evaluation, Preclinical, Glycine, Mice, Nude, 01 natural sciences, Article, Single oral dose, Mice, Structure-Activity Relationship, 03 medical and health sciences, Cell Line, Tumor, Neoplasms, Drug Discovery, medicine, Animals, Humans, Enzyme Inhibitors, 030304 developmental biology, 0303 health sciences, Chemistry, Brain, Myeloid leukemia, Cancer, medicine.disease, Xenograft Model Antitumor Assays, Molecular biology, Isocitrate Dehydrogenase, Rats, 0104 chemical sciences, 010404 medicinal & biomolecular chemistry, Isocitrate dehydrogenase, Microsomes, Liver, Mutagenesis, Site-Directed, Molecular Medicine, Female, Half-Life

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5d6c4e845279737db3495a9974e39ba7
    https://doi.org/10.1021/acs.jmedchem.1c00019

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  3. 3
    Small Molecule Reversible Inhibitors of Bruton's Tyrosine Kinase (BTK): Structure-Activity Relationships Leading to the Identification of 7-(2-Hydroxypropan-2-yl)-4-[2-methyl-3-(4-oxo-3,4-dihydroquinazolin-3-yl)phenyl]-9H-carbazole-1-carboxamide (BMS-935177)

    المؤلفون: Tracy L. Taylor, Douglas G. Batt, Lorell Discenza, ChiehYing J. Chang, Luisa Salter-Cid, Kim W. McIntyre, Myra Beaudoin Bertrand, Percy H. Carter, Yingru Zhang, Qingjie Liu, James R. Burke, Andrew J. Tebben, Zheng Yang, Joel C. Barrish, Rick Rampulla, Aberra Fura, Daniel W. Kukral, Joseph A. Tino, Punit Marathe, Huiping Zhang, Jun Dai, Qing Shi, Arvind Mathur, Kathleen M. Gillooly, Mark A. Pattoli, Mary T. Obermeier, Stacey Skala, Jodi K. Muckelbauer, George V. De Lucca, Rodney Vickery, Celia D’Arienzo

    المصدر: Journal of medicinal chemistry. 59(17)

    مصطلحات موضوعية: 0301 basic medicine, medicine.drug_class, Stereochemistry, Carbazoles, Administration, Oral, Biological Availability, Carboxamide, Crystallography, X-Ray, Permeability, Cell Line, Arthritis, Rheumatoid, 03 medical and health sciences, chemistry.chemical_compound, Mice, Structure-Activity Relationship, 0302 clinical medicine, Dogs, In vivo, Drug Discovery, medicine, Agammaglobulinaemia Tyrosine Kinase, Bruton's tyrosine kinase, Structure–activity relationship, Animals, Humans, Quinazolinones, biology, Carbazole, Protein-Tyrosine Kinases, Small molecule, Arthritis, Experimental, Macaca fascicularis, 030104 developmental biology, chemistry, Cell culture, 030220 oncology & carcinogenesis, Antirheumatic Agents, biology.protein, Microsomes, Liver, Molecular Medicine, Tyrosine kinase

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::76adcd8fa57a42d6c3f428fea7946e0b
    https://pubmed.ncbi.nlm.nih.gov/27531604

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  4. 4
    Identification and Optimization of Pteridinone Toll-like Receptor 7 (TLR7) Agonists for the Oral Treatment of Viral Hepatitis

    المؤلفون: Paul Hrvatin, Jim Zheng, Paul Duatschek, Joseph Hesselgesser, Jessica Jade Chao, Daniel B. Tumas, Gallagher Brian, Randall L. Halcomb, Paul A. Roethle, Michael Graupe, Jason K. Perry, Ryan Mcfadden, Yang Hong, Hui Hon Chung, Bing Lu

    المصدر: Journal of Medicinal Chemistry. 56:7324-7333

    مصطلحات موضوعية: Male, Models, Molecular, Protein Conformation, Drug Evaluation, Preclinical, Administration, Oral, Pharmacology, Antiviral Agents, Substrate Specificity, Mice, Structure-Activity Relationship, Dogs, Hepatitis B, Chronic, Pharmacokinetics, In vivo, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Receptor, Toll-like receptor, Chemistry, Pteridines, TLR7, Hepatitis B, medicine.disease, Rats, Toll-Like Receptor 7, Microsomes, Liver, Molecular Medicine, Female, Viral hepatitis

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a54d0fc30d25240872dcd5a594125125
    https://doi.org/10.1021/jm400815m

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  5. 5
    Lead Optimization of a 4-Aminopyridine Benzamide Scaffold To Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors

    المؤلفون: Sue Sohn, Nico Ghilardi, Priscilla Mantik, Christine Chang, Mercedesz Balazs, Paul Gibbons, Jan Smith, Ivan Peng, Jason DeVoss, Bing-Yan Zhu, Kathy Barrett, Wade S. Blair, Yisong Xiao, Steven Shia, Birong Zhang, Jim Driscoll, Donnie Delarosa, Young G. Shin, Jeremy Murray, Steven Magnuson, Leo Berezhkovsky, Wenqian Yang, Anne van Abbema, Charles Eigenbrot, Lawren C. Wu, Adam R. Johnson, Pawan Bir Kohli, Vickie Tsui, Mark Ultsch, Jason Halladay, Amy Sambrone, Yingjie Lai, Joseph P. Lyssikatos, Yanzhou Liu, Kapil Menghrajani, Jun Liang, Judy Young

    المصدر: Journal of Medicinal Chemistry. 56:4521-4536

    مصطلحات موضوعية: Models, Molecular, Administration, Oral, Aminopyridines, Biological Availability, Pharmacology, Crystallography, X-Ray, Interferon-gamma, Mice, Structure-Activity Relationship, chemistry.chemical_compound, In vivo, Drug Discovery, Animals, Structure–activity relationship, Potency, 4-Aminopyridine, Benzamide, Cell potency, TYK2 Kinase, chemistry.chemical_classification, Gene knockdown, Chemistry, Janus Kinase 3, Stereoisomerism, Janus Kinase 1, Janus Kinase 2, STAT4 Transcription Factor, Interleukin-12, Rats, Enzyme, Biochemistry, Tyrosine kinase 2, Benzamides, Microsomes, Liver, Molecular Medicine, Protein Binding

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::91486c8bd1e5cbb09b64ed7bef1646df
    https://doi.org/10.1021/jm400266t

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  6. 6
    Synthetic Silvestrol Analogues as Potent and Selective Protein Synthesis Inhibitors

    المؤلفون: Patrick O'Hearn, Janid A. Ali, Kelly Slocum, Jitendra D. Belani, Sherri Smith, Tao Liu, Adilah Bahadoor, Andre Lescarbeau, Somarajan J. Nair, Christian C. Fritz, Karen McGovern, Kip A. West, Joseph Helble, Bonnie Tillotson, Martin R. Tremblay, Wylie Andrew A, Vito J. Palombella, Alfredo C. Castro, Stéphane Peluso, James M. Conley, Mark Douglas

    المصدر: Journal of Medicinal Chemistry. 55:8859-8878

    مصطلحات موضوعية: Untranslated region, Antineoplastic Agents, Stereoisomerism, Mice, Structure-Activity Relationship, chemistry.chemical_compound, Genes, Reporter, Cell Line, Tumor, Drug Discovery, Animals, Humans, Structure–activity relationship, Benzofuran, Luciferases, ADME, Protein Synthesis Inhibitors, Reporter gene, Natural product, Translation (biology), Triterpenes, chemistry, Biochemistry, Microsomes, Liver, Molecular Medicine, Drug Screening Assays, Antitumor, 5' Untranslated Regions

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ca8e686d0a86b9c6d0b9d6e0f79d708d
    https://doi.org/10.1021/jm3011542

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  7. 7
    Optimization of Propafenone Analogues as Antimalarial Leads

    المؤلفون: Andrew Lemoff, Michele Connelly, David J. Lowes, Joseph L. DeRisi, Fangyi Zhu, W. Armand Guiguemde, R. Kiplin Guy, Martina Sigal, Julie Clark, Emily Wilson

    المصدر: Journal of Medicinal Chemistry. 54:7477-7485

    مصطلحات موضوعية: Male, Drug, media_common.quotation_subject, Plasmodium falciparum, Drug Resistance, Propafenone, Drug resistance, In Vitro Techniques, Pharmacology, Ion Channels, Permeability, Article, Cell Line, Antimalarials, Mice, Structure-Activity Relationship, Parasitic Sensitivity Tests, Pharmacokinetics, parasitic diseases, Drug Discovery, medicine, Animals, Humans, Structure–activity relationship, Potency, media_common, biology, Chemistry, Membranes, Artificial, Stereoisomerism, biology.organism_classification, Multiple drug resistance, Solubility, Microsomes, Liver, Molecular Medicine, Female, medicine.drug

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e0e0b4dfebd42fbf8f4054cff010759
    https://doi.org/10.1021/jm2005546

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  8. 8
    2,7-Disubstituted-pyrrolo[2,1-f][1,2,4]triazines: New Variant of an Old Template and Application to the Discovery of Anaplastic Lymphoma Kinase (ALK) Inhibitors with in Vivo Antitumor Activity

    المؤلفون: Mark S. Albom, Bruce D. Dorsey, Joseph G. Lisko, Mangeng Cheng, Bruce Ruggeri, Arup K. Ghose, Eugen F. Mesaros, Weihua Wan, Mark A. Ator, Matthew R. Quail, Zeqi Huang, Diane E. Gingrich, Tho V. Thieu, Gregory J. Wells, Thelma S. Angeles, Gregory R. Ott, Lisa D. Aimone, Lihui Lu

    المصدر: Journal of Medicinal Chemistry. 54:6328-6341

    مصطلحات موضوعية: Models, Molecular, Cell Membrane Permeability, Transplantation, Heterologous, Antineoplastic Agents, Mice, SCID, In Vitro Techniques, Rats, Sprague-Dawley, Mice, Structure-Activity Relationship, chemistry.chemical_compound, In vivo, Cell Line, Tumor, hemic and lymphatic diseases, Drug Discovery, medicine, Animals, Humans, Anaplastic lymphoma kinase, Structure–activity relationship, Anaplastic Lymphoma Kinase, Pyrroles, Anaplastic large-cell lymphoma, Triazine, Sulfonamides, Triazines, Chemistry, Kinase, Receptor Protein-Tyrosine Kinases, Bridged Bicyclo Compounds, Heterocyclic, medicine.disease, Rats, Transplantation, Diaminopyrimidine, Biochemistry, Microsomes, Liver, Lymphoma, Large-Cell, Anaplastic, Molecular Medicine, Drug Screening Assays, Antitumor, Neoplasm Transplantation

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4ff1dc2c02c706eed915e53603283891
    https://doi.org/10.1021/jm200758k

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  9. 9
    Structure–Activity Relationships of Antitubercular Nitroimidazoles. 3. Exploration of the Linker and Lipophilic Tail of ((S)-2-Nitro-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazin-6-yl)-(4-trifluoromethoxybenzyl)amine (6-Amino PA-824)

    المؤلفون: Yong Sok Lee, Clifton E. Barry, Young Hwan Ha, Jan Jiricek, Thomas H. Keller, Pornwaratt Niyomrattanakit, Sindhu Ravindran, Thomas Dick, Michael Goodwin, Véronique Dartois, Tathagata Mukherjee, Suresh B. Lakshminarayana, Ujjini H. Manjunatha, Helena I. Boshoff, Joseph Cherian, Inhee Choi, Ramandeep Singh, Amit Nayyar

    المصدر: Journal of Medicinal Chemistry. 54:5639-5659

    مصطلحات موضوعية: Metabolic Clearance Rate, Stereochemistry, Antitubercular Agents, Drug Evaluation, Preclinical, Microbial Sensitivity Tests, Article, Substrate Specificity, Mice, Structure-Activity Relationship, Nitroreductase, Bacterial Proteins, Drug Discovery, Animals, Humans, Tuberculosis, Structure–activity relationship, Prodrugs, Molecular Structure, Chemistry, Mycobacterium tuberculosis, Nitroreductases, Prodrug, In vitro, Kinetics, Nitroimidazoles, Microsomes, Liver, Microsome, Nitro, Molecular Medicine, Amine gas treating, Linker

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99931f461d7a119cb7d418b72de9bac0
    https://doi.org/10.1021/jm1010644

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  10. 10
    Optimization of the in Vitro Cardiac Safety of Hydroxamate-Based Histone Deacetylase Inhibitors

    المؤلفون: Chen Christine Hiu-Tung, Remiszewski Stacy W, Jianmei Fan, Alex Fekete, Brant Firestone, Joseph D. Growney, Christopher T. Meta, Joe Eckman, Dyuti Majumdar, Ping Wang, Peter Atadja, Vinita Uttamsingh, Liping Zhou, Laszlo Urban, Qiang Lu, Meier Hsu, Suzanne Skolnik, Lei Jiang, Tim Ramsey, Martin Traebert, Yan Yan-Neale, Minying Pu, Julie Flynn, Lawrence Blas Perez, Yung-Mae Yao, Xueying Cao, Franco Lombardo, Steven Whitebread, Mats Holmqvist, Lewis Whitehead, Young Shin Cho, Paul Kwon, N Davis, Jack Green, Daniel Jansson, Michael Shultz, Gang Liu

    المصدر: Journal of Medicinal Chemistry. 54:4752-4772

    مصطلحات موضوعية: Models, Molecular, ERG1 Potassium Channel, congenital, hereditary, and neonatal diseases and abnormalities, Patch-Clamp Techniques, Transplantation, Heterologous, hERG, Mice, Nude, Antineoplastic Agents, In Vitro Techniques, Pharmacology, Hydroxamic Acids, Rats, Sprague-Dawley, Mice, Radioligand Assay, Structure-Activity Relationship, Drug Discovery, Animals, Humans, Structure–activity relationship, Tissue Distribution, cardiovascular diseases, Homology modeling, Ion channel, Acrylamides, biology, Chemistry, Stereoisomerism, HCT116 Cells, Ether-A-Go-Go Potassium Channels, In vitro, Rats, Histone Deacetylase Inhibitors, Transplantation, Microsomes, Liver, biology.protein, Molecular Medicine, Histone deacetylase, Drug Screening Assays, Antitumor, Pharmacophore, Neoplasm Transplantation, Half-Life

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c444090ceb6d32a590072a95df83c006
    https://doi.org/10.1021/jm200388e

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