يعرض 1 - 10 نتائج من 40 نتيجة بحث عن '"Dac M, Dinh"', وقت الاستعلام: 1.07s تنقيح النتائج
  1. 1
    Optimization of Orally Bioavailable Enhancer of Zeste Homolog 2 (EZH2) Inhibitors Using Ligand and Property-Based Design Strategies: Identification of Development Candidate (R)-5,8-Dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497)

    المؤلفون: Michael R. Collins, Robert Steven Kania, Connie Fan, Sutton Scott Channing, Dominique Verhelle, Kephart Susan Elizabeth, Martin James Wythes, Shuiwang Wang, Karen A. Maegley, Lisa Nguyen, Daniel Tyler Richter, A.E. Stewart, Pei-Pei Kung, Buwen Huang, Shikhar Sharma, Shinji Yamazaki, Ya-Li Deng, Rita Grantner, Patrick Bingham, Robert Arnold Kumpf, Penney Khamphavong, Jinjiang Zhu, Dac M. Dinh, Manfred Kraus, Wei Liu, Sean Uryu, Jillian E. Spangler, Wenyue Hu, Hui Wang, Robert A. Rollins, Cody Krivacic, Zehnder Luke Raymond, Neal W. Sach, Alexei Brooun, John Sherrill, Shijian Ren, Martin A. Edwards, Huichun Zhu, Ketan S. Gajiwala, Shuibo Xin, Hovhannes J. Gukasyan

    المصدر: Journal of Medicinal Chemistry. 61:650-665

    مصطلحات موضوعية: 0301 basic medicine, Chemistry, Stereochemistry, Ligand (biochemistry), 03 medical and health sciences, chemistry.chemical_compound, 030104 developmental biology, In vivo, Drug Discovery, Lactam, Molecular Medicine, Moiety, Molecule, Solubility, Lead compound, ADME

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::f30f1b1d2d6acfd5a3cfe913d0c1179d
    https://doi.org/10.1021/acs.jmedchem.7b01375

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  2. 2
    Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR

    المؤلفون: Chengyi Zhang, Sujin Cho-Schultz, Tran Khanh Tuan, Manli Shi, Rose Ann Ferre, Sherry Niessen, Sajiv Krishnan Nair, Douglas Carl Behenna, Dac M. Dinh, Elaine E. Tseng, Theodore O. Johnson, Cheng Hengmiao, Ru Zhou, Michael Zientek, T. Eric Ballard, Brion W. Murray, Suvi T. M. Orr, James Solowiej, Jennifer Lafontaine, Jean Joo Matthews, Scott L. Weinrich, Paolo Vicini, Deal Judith G, Longqing Liu, John Charles Kath, Pairish Mason Alan, Simon Paul Planken, Louise Bernier, Deepak Dalvie, Yiqin Luo, Martin Paul Edwards, Asako Nagata, Hong Shen, Neal W. Sach, Yuli Wang, Ketan S. Gajiwala, Shuibo Xin, Simon Bailey, Chau Almaden, Robert Steven Kania, Michelle Hemkens

    المصدر: Journal of Medicinal Chemistry. 60:3002-3019

    مصطلحات موضوعية: 0301 basic medicine, Mutation, biology, Chemistry, Mutant, Wild type, medicine.disease_cause, Molecular biology, respiratory tract diseases, 03 medical and health sciences, T790M, 030104 developmental biology, Drug Discovery, biology.protein, medicine, Molecular Medicine, Kinome, Epidermal growth factor receptor, Erlotinib, ADME, medicine.drug

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::b35c90cb7e71bbfee825479df1f470d5
    https://doi.org/10.1021/acs.jmedchem.6b01894

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  3. 3
    Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

    المؤلفون: Marlena Walls, Tod Smeal, Suvi T. M. Orr, Zhengyu Liu, Cheng Hengmiao, Shuiwang Wang, Kephart Susan Elizabeth, Jean Joo Matthews, Rose Ann Ferre, Neal W. Sach, Scott L. Weinrich, Doug Behenna, Sherry Niessen, Sangita M. Baxi, Deepak Dalvie, Sujin Cho-Schultz, Dac M. Dinh, Kevin Ryan, Jim Solowiej, Elaine E. Tseng, Simon Paul Planken, Sajiv Krishnan Nair, Brion W. Murray, Jun Li Feng, Jennifer Lafontaine, Pairish Mason Alan, Shijian Ren, Michelle Hemkens, Shuibo Xin, Mehran Jalaie, Tran Khanh Tuan, Robert Steven Kania, Sutton Scott Channing, William F. Vernier, Kevin K.-C. Liu, Amy Jackson-Fisher, Beth Lunney, Min-Jean Yin, Ketan S. Gajiwala, Asako Nagata, Haiwei Xu, Michael Zientek, Ru Zhou, Daniel Tyler Richter, Simon Bailey, Martin Paul Edwards, Martha A. Ornelas, Chau Almaden, John Charles Kath, Hong Shen, Theodore O. Johnson

    المصدر: Journal of Medicinal Chemistry. 59:2005-2024

    مصطلحات موضوعية: 0301 basic medicine, Mutation, 010405 organic chemistry, Stereochemistry, Chemistry, Mutant, medicine.disease_cause, 01 natural sciences, respiratory tract diseases, 0104 chemical sciences, 03 medical and health sciences, T790M, 030104 developmental biology, Gefitinib, Protein kinase domain, Drug Discovery, Cancer research, medicine, Molecular Medicine, Potency, Reactivity (chemistry), Erlotinib, medicine.drug

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_________::dcd650965ee5ecc3e2b378a7f2542e1b
    https://doi.org/10.1021/acs.jmedchem.5b01633

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  4. 4
    PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models

    المؤلفون: Wenyue Hu, Rosa L. Frias, Hovhannes J. Gukasyan, Alice T. Shaw, Valeria Fantin, Ryohei Katayama, Nathan V. Lee, Ruth W. Tang, Timothy Affolter, Eugene Lifshits, Ted William Johnson, Divya Bezwada, David P. Kodack, Lars D. Engstrom, Hieu Lam, Sidra Mahmood, Tod Smeal, Luc Friboulet, Rakesh K. Jain, Hui Wang, Melissa West, Dac M. Dinh, Bhushankumar Patel, Qiuhua Li, Konstantinos Tsaparikos, Helen Y. Zou, Justine L. Lam, Sergei Timofeevski, Shinji Yamazaki, Patrick B. Lappin, Justin F. Gainor, Shibing Deng, Jinwei Wang

    المصدر: Cancer Cell. 28:70-81

    مصطلحات موضوعية: Alectinib, Cancer Research, Mutation, Brigatinib, Ceritinib, business.industry, Cell Biology, Drug resistance, Pharmacology, medicine.disease_cause, Lorlatinib, 3. Good health, Oncology, hemic and lymphatic diseases, medicine, ROS1, Anaplastic lymphoma kinase, business, medicine.drug

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::bf01b5d870097f37627bdb071f98ad35
    https://doi.org/10.1016/j.ccell.2015.05.010

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  5. 5
    Design, Synthesis, and Evaluation of NO-Donor Containing Carbonic Anhydrase Inhibitors To Lower Intraocular Pressure

    المؤلفون: Saurabh Mehta, Hovhannes J. Gukasyan, Morena Cobbs, Martin Paul Edwards, Dac M. Dinh, Paul F. Richardson, Jennifer Lafontaine, Rui Eugene Yuanjin, Brian Douglas Patterson, Qinhua Huang, D.A. Rewolinski

    المصدر: Journal of Medicinal Chemistry. 58:2821-2833

    مصطلحات موضوعية: Male, Intraocular pressure, genetic structures, Brinzolamide, Thiazines, Thiophenes, Pharmacology, No donors, Nitric oxide, chemistry.chemical_compound, Dorzolamide, Carbonic anhydrase, Drug Discovery, medicine, Animals, Nitric Oxide Donors, Carbonic Anhydrase Inhibitors, Intraocular Pressure, chemistry.chemical_classification, Sulfonamides, biology, Chemistry, Glaucoma, eye diseases, Enzyme, Design synthesis, Drug Design, biology.protein, Molecular Medicine, Rabbits, sense organs, medicine.drug

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5aa62e66b730d4838dec71bff4fdaf1
    https://doi.org/10.1021/acs.jmedchem.5b00043

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  6. 6
    Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR

    المؤلفون: Simon, Planken, Douglas C, Behenna, Sajiv K, Nair, Theodore O, Johnson, Asako, Nagata, Chau, Almaden, Simon, Bailey, T Eric, Ballard, Louise, Bernier, Hengmiao, Cheng, Sujin, Cho-Schultz, Deepak, Dalvie, Judith G, Deal, Dac M, Dinh, Martin P, Edwards, Rose Ann, Ferre, Ketan S, Gajiwala, Michelle, Hemkens, Robert S, Kania, John C, Kath, Jean, Matthews, Brion W, Murray, Sherry, Niessen, Suvi T M, Orr, Mason, Pairish, Neal W, Sach, Hong, Shen, Manli, Shi, James, Solowiej, Khanh, Tran, Elaine, Tseng, Paolo, Vicini, Yuli, Wang, Scott L, Weinrich, Ru, Zhou, Michael, Zientek, Longqing, Liu, Yiqin, Luo, Shuibo, Xin, Chengyi, Zhang, Jennifer, Lafontaine

    المصدر: Journal of medicinal chemistry. 60(7)

    مصطلحات موضوعية: Models, Molecular, Acrylamides, Lung Neoplasms, Pyrrolidines, Halogenation, Rats, ErbB Receptors, Molecular Docking Simulation, Mice, Dogs, Carcinoma, Non-Small-Cell Lung, Cell Line, Tumor, Drug Design, Mutation, Animals, Humans, Lung, Protein Kinase Inhibitors

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=pmid________::424669cfffca599d5b525ea1e0d9fe2e
    https://pubmed.ncbi.nlm.nih.gov/28287730

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  7. 7
    Discovery of (10R)-7-Amino-12-fluoro-2,10,16-trimethyl-15-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h][2,5,11]-benzoxadiazacyclotetradecine-3-carbonitrile (PF-06463922), a Macrocyclic Inhibitor of Anaplastic Lymphoma Kinase (ALK) and c-ros Oncogene 1 (ROS1) with Preclinical Brain Exposure and Broad-Spectrum Potency against ALK-Resistant Mutations

    المؤلفون: Sergei Timofeevski, Lars D. Engstrom, Mingying He, Michael R. Collins, Martin Paul Edwards, Phuong Le, Graham L. Smith, John Charles Kath, Helen Y. Zou, Deal Judith G, Ya-Li Deng, Robert Steven Kania, Benjamin J. Burke, Cynthia Louise Palmer, Huichun Zhu, A.E. Stewart, Hieu Lam, Dac M. Dinh, Simon Bailey, Jacqui Elizabeth Hoffman, Neal W. Sach, Robert Louis Hoffman, Qinhua Huang, J. Jean Cui, Alexei Brooun, Wei Liu, Laura Lingardo, Tod Smeal, Ted William Johnson, Michele McTigue, Justine L. Lam, Jinjiang Zhu, Paul F. Richardson

    المصدر: Journal of Medicinal Chemistry. 57:4720-4744

    مصطلحات موضوعية: Models, Molecular, Lactams, Brigatinib, Lactams, Macrocyclic, Aminopyridines, Antineoplastic Agents, Crystallography, X-Ray, Mice, Structure-Activity Relationship, Proto-Oncogene Proteins, hemic and lymphatic diseases, Drug Discovery, medicine, ROS1, Animals, Humans, Anaplastic lymphoma kinase, Anaplastic Lymphoma Kinase, ADME, Crizotinib, Chemistry, Drug discovery, Brain, Receptor Protein-Tyrosine Kinases, Stereoisomerism, Protein-Tyrosine Kinases, Lorlatinib, Rats, Drug Resistance, Neoplasm, Lipophilic efficiency, Mutation, Microsomes, Liver, NIH 3T3 Cells, Cancer research, Pyrazoles, Molecular Medicine, medicine.drug

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a88513bc93ec9da81fd3688f6b55fb99
    https://doi.org/10.1021/jm500261q

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  8. 8
    Design of Potent and Selective Inhibitors to Overcome Clinical Anaplastic Lymphoma Kinase Mutations Resistant to Crizotinib

    المؤلفون: Tod Smeal, Wei Liu, Huichun Zhu, Simon Bailey, Michael R. Collins, A.E. Stewart, Jacqui Elizabeth Hoffman, Lars D. Engstrom, Graham L. Smith, J. Jean Cui, Ya-Li Deng, Benjamin J. Burke, Laura Lingardo, Phuong Le, Andrew Simon Cook, Konstantinos Tsaparikos, Hieu Lam, Jinjiang Zhu, Ted William Johnson, Neal W. Sach, Dac M. Dinh, Robert Louis Hoffman, Mingying He, Hui Wang, Alexei Brooun, Dack Kevin Neil, Qinhua Huang, Sergei Timofeevski, Deal Judith G, Justine L. Lam, Qiuhua Li, Hong Shen, Melissa West Lu, Michele McTigue, Paul F. Richardson, Kevin D. Bunker, Robert Steven Kania, Martin Paul Edwards, Helen Y. Zou, Cynthia Louise Palmer, Patrick S. Johnson

    المصدر: Journal of Medicinal Chemistry. 57:1170-1187

    مصطلحات موضوعية: Drug, Pyridines, media_common.quotation_subject, Drug resistance, Pharmacology, Crizotinib, hemic and lymphatic diseases, Drug Discovery, medicine, Humans, Point Mutation, Anaplastic lymphoma kinase, Anaplastic Lymphoma Kinase, Protein Kinase Inhibitors, media_common, Chemistry, Point mutation, Receptor Protein-Tyrosine Kinases, medicine.disease, Protein kinase domain, Drug Resistance, Neoplasm, Cell culture, Cancer research, Pyrazoles, Molecular Medicine, Progressive disease, medicine.drug

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6f25cdb3a3b4202005c75976a5f6a5ac
    https://doi.org/10.1021/jm401805h

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  9. 9
    Design and Synthesis of Pyridone-Containing 3,4-Dihydroisoquinoline-1(2H)-ones as a Novel Class of Enhancer of Zeste Homolog 2 (EZH2) Inhibitors

    المؤلفون: Hovhannes J. Gukasyan, Michael R. Collins, Sutton Scott Channing, Kephart Susan Elizabeth, Shinji Yamazaki, Sacha Ninkovic, Simon Bergqvist, Fen Wang, Robert Arnold Kumpf, Michael Ryskin, Patrick Bingham, Pei-Pei Kung, Dominique Verhelle, Brian Yip, Karen A. Maegley, Robert A. Rollins, Peter A. Wells, Martha A. Ornelas, Buwen Huang, Valeria Fantin, Xiu Yu, Stephanie Scales, Wade Diehl, Indrawan James Mcalpine, Cody Krivacic, Mei Cui, Lisa Nguyen, Wenyue Hu, Tatlock John H, Dac M. Dinh, Martin James Wythes, Connie Fan, Gary Li, Martin Paul Edwards, Rui Eugene Yuanjin, John F. Braganza, Zehnder Luke Raymond, Wei-Guo Zhang

    المصدر: Journal of medicinal chemistry. 59(18)

    مصطلحات موضوعية: 0301 basic medicine, Models, Molecular, Lactams, Stereochemistry, Pyridones, Antineoplastic Agents, Mice, SCID, 03 medical and health sciences, chemistry.chemical_compound, Mice, In vivo, Amide, Cell Line, Tumor, Neoplasms, Drug Discovery, Potency, Moiety, Animals, Humans, Enhancer of Zeste Homolog 2 Protein, Ligand efficiency, Isoquinolines, 030104 developmental biology, chemistry, Lipophilic efficiency, Cyclization, Drug Design, Lactam, Molecular Medicine, Female, Linker

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f62bbe5fc41702928ba23fd544b9fadd
    https://pubmed.ncbi.nlm.nih.gov/27936698

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  10. 10
    Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants

    المؤلفون: Hengmiao, Cheng, Sajiv K, Nair, Brion W, Murray, Chau, Almaden, Simon, Bailey, Sangita, Baxi, Doug, Behenna, Sujin, Cho-Schultz, Deepak, Dalvie, Dac M, Dinh, Martin P, Edwards, Jun Li, Feng, Rose Ann, Ferre, Ketan S, Gajiwala, Michelle D, Hemkens, Amy, Jackson-Fisher, Mehran, Jalaie, Ted O, Johnson, Robert S, Kania, Susan, Kephart, Jennifer, Lafontaine, Beth, Lunney, Kevin K-C, Liu, Zhengyu, Liu, Jean, Matthews, Asako, Nagata, Sherry, Niessen, Martha A, Ornelas, Suvi T M, Orr, Mason, Pairish, Simon, Planken, Shijian, Ren, Daniel, Richter, Kevin, Ryan, Neal, Sach, Hong, Shen, Tod, Smeal, Jim, Solowiej, Scott, Sutton, Khanh, Tran, Elaine, Tseng, William, Vernier, Marlena, Walls, Shuiwang, Wang, Scott L, Weinrich, Shuibo, Xin, Haiwei, Xu, Min-Jean, Yin, Michael, Zientek, Ru, Zhou, John C, Kath

    المصدر: Journal of medicinal chemistry. 59(5)

    مصطلحات موضوعية: Models, Molecular, Lung Neoplasms, Dose-Response Relationship, Drug, Molecular Structure, ErbB Receptors, Structure-Activity Relationship, Pyrimidines, Carcinoma, Non-Small-Cell Lung, Drug Discovery, Mutation, Tumor Cells, Cultured, Humans, Mutant Proteins, Pyrroles, Protein Kinase Inhibitors

    URL الوصول: https://explore.openaire.eu/search/publication?articleId=pmid________::f69cf3e766e492ce164cc24ad82b59de
    https://pubmed.ncbi.nlm.nih.gov/26756222

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