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heterocyclic compounds, 2-ring - pharmacology (382) 382
science & technology (326) 326
life sciences & biomedicine (306) 306
humans (291) 291
animals (278) 278
heterocyclic compounds, 2-ring - chemistry (239) 239
heterocyclic compounds, 2-ring - chemical synthesis (141) 141
pharmacology & pharmacy (141) 141
biological and medical sciences (132) 132
structure-activity relationship (128) 128
mice (119) 119
male (115) 115
medical sciences (113) 113
molecular structure (100) 100
cell line, tumor (98) 98
pharmacology. drug treatments (97) 97
female (91) 91
chemistry (89) 89
chemistry, medicinal (80) 80
physical sciences (78) 78
rats (72) 72
biochemistry & molecular biology (70) 70
antineoplastic agents - pharmacology (66) 66
dose-response relationship, drug (65) 65
heterocyclic compounds, 2-ring - therapeutic use (60) 60
heterocyclic compounds, 2-ring - pharmacokinetics (51) 51
analysis (49) 49
models, molecular (49) 49
cell proliferation - drug effects (48) 48
oncology (47) 47
antineoplastic agents - chemistry (44) 44
enzyme inhibitors - pharmacology (42) 42
apoptosis - drug effects (39) 39
heterocyclic compounds, 2-ring - isolation & purification (39) 39
heterocyclic compounds, 2-ring - administration & dosage (37) 37
drug design (36) 36
rats, sprague-dawley (34) 34
apoptosis (31) 31
cell survival - drug effects (31) 31
pyrazoles - pharmacology (31) 31
antineoplastic agents - chemical synthesis (30) 30
cell biology (30) 30
drug screening assays, antitumor (30) 30
magnetic resonance spectroscopy (30) 30
microbial sensitivity tests (30) 30
protein kinase inhibitors - pharmacology (30) 30
research (30) 30
amidines - pharmacology (29) 29
cell line (29) 29
chemistry, organic (29) 29
crystallography, x-ray (29) 29
protein binding (29) 29
fundamental and applied biological sciences. psychology (28) 28
heterocyclic compounds, 2-ring - metabolism (28) 28
thiazoles - pharmacology (27) 27
adult (26) 26
chemistry, multidisciplinary (26) 26
proteins (26) 26
cancer (25) 25
administration, oral (24) 24
antineoplastic agents (24) 24
cells, cultured (24) 24
heterocyclic compounds, 2-ring (24) 24
pyrazoles - chemistry (24) 24
spiro compounds - pharmacology (24) 24
stereoisomerism (24) 24
binding sites (23) 23
inhibitors (23) 23
inhibitory concentration 50 (23) 23
ligands (23) 23
anti-bacterial agents - pharmacology (22) 22
disease models, animal (22) 22
dogs (22) 22
gene expression (22) 22
nitric oxide synthase - antagonists & inhibitors (22) 22
organic chemistry (22) 22
pyridines - pharmacology (22) 22
signal transduction (22) 22
furans - pharmacology (21) 21
mice, inbred c57bl (21) 21
xenograft model antitumor assays (21) 21
heterocyclic compounds, 2-ring - toxicity (20) 20
kinases (20) 20
middle aged (20) 20
signal transduction - drug effects (20) 20
cell cycle (19) 19
double-blind method (19) 19
heterocyclic compounds (19) 19
mice, inbred balb c (19) 19
mutation (19) 19
neuropharmacology (19) 19
sulfonamides - pharmacology (19) 19
anti-bacterial agents - chemistry (18) 18
antibiotics. antiinfectious agents. antiparasitic agents (18) 18
molecular conformation (18) 18
pharmacology (18) 18
piperazines - pharmacology (18) 18
protein kinase inhibitors - chemistry (18) 18
pyrimidines - pharmacology (18) 18
time factors (18) 18
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1. Full Text Design, Synthesis, and Evaluation of Thiophene[3,2‑d]pyrimidine Derivatives as HIV‑1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles
by Kang, Dongwei and Fang, Zengjun and Li, Zhenyu and Huang, Boshi and Zhang, Heng and Lu, Xueyi and Xu, Haoran and Zhou, Zhongxia and Ding, Xiao and Daelemans, Dirk and De Clercq, Erik and Pannecouque, Christophe and Zhan, Peng and Liu, Xinyong
Journal of medicinal chemistry, ISSN 0022-2623, 09/2016, Volume 59, Issue 17, pp. 7991 - 8007
Anti-HIV Agents - pharmacology | Pyrimidines - chemical synthesis | HIV Reverse Transcriptase - antagonists & inhibitors | Humans | Drug Resistance, Viral | Reverse Transcriptase Inhibitors - pharmacology | Male | Structure-Activity Relationship | Anti-HIV Agents - chemical synthesis | Pyrimidines - chemistry | Reverse Transcriptase Inhibitors - chemistry | Reverse Transcriptase Inhibitors - chemical synthesis | Reverse Transcriptase Inhibitors - pharmacokinetics | Sulfonamides - chemistry | Heterocyclic Compounds, 2-Ring - chemistry | Thiophenes - pharmacology | Heterocyclic Compounds, 2-Ring - pharmacokinetics | Pyrimidines - pharmacology | HIV-1 - genetics | Sulfonamides - pharmacology | Rats, Sprague-Dawley | Sulfonamides - pharmacokinetics | Heterocyclic Compounds, 2-Ring - pharmacology | Sulfonamides - chemical synthesis | Thiophenes - chemical synthesis | Thiophenes - pharmacokinetics | Anti-HIV Agents - chemistry | Animals | Anti-HIV Agents - pharmacokinetics | Cell Line, Tumor | Pyrimidines - pharmacokinetics | HIV-1 - enzymology | Mice | Molecular Docking Simulation | Mutation | Thiophenes - chemistry | Heterocyclic Compounds, 2-Ring - chemical synthesis | Index Medicus
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2. Full Text Omarigliptin (MK-3102): A Novel Long-Acting DPP‑4 Inhibitor for Once-Weekly Treatment of Type 2 Diabetes
by Biftu, Tesfaye and Sinha-Roy, Ranabir and Chen, Ping and Qian, Xiaoxia and Feng, Dennis and Kuethe, Jeffrey T and Scapin, Giovanna and Gao, Ying Duo and Yan, Youwei and Krueger, Davida and Bak, Annette and Eiermann, George and He, Jiafang and Cox, Jason and Hicks, Jacqueline and Lyons, Kathy and He, Huaibing and Salituro, Gino and Tong, Sharon and Patel, Sangita and Doss, George and Petrov, Aleksandr and Wu, Joseph and Xu, Shiyao Sherrie and Sewall, Charles and Zhang, Xiaoping and Zhang, Bei and Thornberry, Nancy A and Weber, Ann E and Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Journal of medicinal chemistry, ISSN 0022-2623, 04/2014, Volume 57, Issue 8, pp. 3205 - 3212
Pyrans - chemical synthesis | Hypoglycemic Agents - pharmacokinetics | Dipeptidyl-Peptidase IV Inhibitors - toxicity | Humans | Pyrans - toxicity | Structure-Activity Relationship | Heterocyclic Compounds, 2-Ring - pharmacokinetics | Dipeptidyl-Peptidase IV Inhibitors - pharmacology | Heterocyclic Compounds, 2-Ring - pharmacology | Hypoglycemic Agents - pharmacology | Hypoglycemic Agents - toxicity | Dipeptidyl-Peptidase IV Inhibitors - chemical synthesis | Heterocyclic Compounds, 2-Ring - toxicity | Pyrans - pharmacokinetics | Animals | Dipeptidyl-Peptidase IV Inhibitors - pharmacokinetics | Hypoglycemic Agents - chemical synthesis | Diabetes Mellitus, Type 2 - drug therapy | Heterocyclic Compounds, 2-Ring - chemical synthesis | Pyrans - pharmacology | Index Medicus | 60 APPLIED LIFE SCIENCES | INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY
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3. Full Text N-Fused Imidazoles As Novel Anticancer Agents That Inhibit Catalytic Activity of Topoisomerase IIα and Induce Apoptosis in G1/S Phase
by Baviskar, Ashish T and Madaan, Chetna and Preet, Ranjan and Mohapatra, Purusottam and Jain, Vaibhav and Agarwal, Amit and Guchhait, Sankar K and Kundu, Chanakya N and Banerjee, Uttam C and Bharatam, Prasad V
Journal of medicinal chemistry, ISSN 0022-2623, 07/2011, Volume 54, Issue 14, pp. 5013 - 5030
Apoptosis - drug effects | Antineoplastic Agents - chemical synthesis | Humans | Imidazoles - chemistry | Cercopithecus aethiops | Structure-Activity Relationship | Topoisomerase II Inhibitors - chemistry | S Phase | HEK293 Cells | Antineoplastic Agents - pharmacology | Topoisomerase II Inhibitors - chemical synthesis | Imidazoles - chemical synthesis | Intercalating Agents - chemical synthesis | Binding Sites | Vero Cells | Cell Survival - drug effects | Antigens, Neoplasm | DNA-Binding Proteins - antagonists & inhibitors | Heterocyclic Compounds, 2-Ring - chemistry | Etoposide - pharmacology | Models, Molecular | Imidazoles - pharmacology | Intercalating Agents - pharmacology | Topoisomerase II Inhibitors - pharmacology | Antineoplastic Agents - chemistry | Intercalating Agents - chemistry | Molecular Dynamics Simulation | Heterocyclic Compounds, 2-Ring - pharmacology | Cell Movement - drug effects | G1 Phase | Animals | Cell Line, Tumor | Adenosine Triphosphatases - chemistry | DNA Topoisomerases, Type II | Fluorouracil - pharmacology | Adenosine Triphosphate - chemistry | Heterocyclic Compounds, 2-Ring - chemical synthesis | Drug Screening Assays, Antitumor | Index Medicus
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4. Full Text The potent BACE1 inhibitor LY2886721 elicits robust central Aβ pharmacodynamic responses in mice, dogs, and humans
by May, Patrick C and Willis, Brian A and Lowe, Stephen L and Dean, Robert A and Monk, Scott A and Cocke, Patrick J and Audia, James E and Boggs, Leonard N and Borders, Anthony R and Brier, Richard A and Calligaro, David O and Day, Theresa A and Ereshefsky, Larry and Erickson, Jon A and Gevorkyan, Hykop and Gonzales, Celedon R and James, Douglas E and Jhee, Stanford S and Komjathy, Steven F and Li, Linglin and Lindstrom, Terry D and Mathes, Brian M and Martényi, Ferenc and Sheehan, Scott M and Stout, Stephanie L and Timm, David E and Vaught, Grant M and Watson, Brian M and Winneroski, Leonard L and Yang, Zhixiang and Mergott, Dustin J
The Journal of neuroscience, ISSN 0270-6474, 01/2015, Volume 35, Issue 3, pp. 1199 - 1210
BACE1 | Clinical trial | Amyloid beta | Alzheimer’s disease | Nonclinical animal model | Neurosciences | Neurosciences & Neurology | Life Sciences & Biomedicine | Science & Technology | Picolinic Acids - pharmacology | Aspartic Acid Endopeptidases - antagonists & inhibitors | Protease Inhibitors - pharmacokinetics | Humans | Alzheimer Disease - drug therapy | Heterocyclic Compounds, 2-Ring - pharmacokinetics | Amyloid beta-Peptides - blood | Heterocyclic Compounds, 2-Ring - pharmacology | Protease Inhibitors - pharmacology | Animals | Heterocyclic Compounds, 2-Ring - therapeutic use | Picolinic Acids - therapeutic use | Picolinic Acids - pharmacokinetics | Amyloid beta-Peptides - metabolism | Dogs | Amyloid beta-Peptides - cerebrospinal fluid | Mice | Amyloid Precursor Protein Secretases - antagonists & inhibitors | Protease Inhibitors - therapeutic use | Disease Models, Animal | Index Medicus | clinical trial | nonclinical animal model | Alzheimer's disease | amyloid beta
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5. Full Text Design and Synthesis of a Pan-Janus Kinase Inhibitor Clinical Candidate (PF-06263276) Suitable for Inhaled and Topical Delivery for the Treatment of Inflammatory Diseases of the Lungs and Skin
by Jones, Peter and Storer, R. Ian and Sabnis, Yogesh A and Wakenhut, Florian M and Whitlock, Gavin A and England, Katherine S and Mukaiyama, Takasuke and Dehnhardt, Christoph M and Coe, Jotham W and Kortum, Steve W and Chrencik, Jill E and Brown, David G and Jones, Rhys M and Murphy, John R and Yeoh, Thean and Morgan, Paul and Kilty, Iain and Argonne National Lab. (ANL), Argonne, IL (United States)
Journal of medicinal chemistry, ISSN 0022-2623, 01/2017, Volume 60, Issue 2, pp. 767 - 786
Phosphorylation | Indazoles - chemical synthesis | Humans | Microsomes, Liver - metabolism | Crystallography, X-Ray | Administration, Cutaneous | Hepatocytes - metabolism | Indazoles - administration & dosage | Lung Diseases - drug therapy | Janus Kinase 3 - antagonists & inhibitors | Heterocyclic Compounds, 2-Ring - toxicity | Drug Design | Anti-Inflammatory Agents - administration & dosage | Binding Sites | Janus Kinase 2 - antagonists & inhibitors | Protein Kinase Inhibitors - chemical synthesis | Anti-Inflammatory Agents - pharmacology | Anti-Inflammatory Agents - toxicity | Heterocyclic Compounds, 2-Ring - administration & dosage | Solubility | Administration, Inhalation | Rats | Skin Diseases - drug therapy | Janus Kinase 1 - antagonists & inhibitors | Heterocyclic Compounds, 2-Ring - pharmacology | Indazoles - pharmacology | Janus Kinases - antagonists & inhibitors | Protein Kinase Inhibitors - administration & dosage | Animals | Indazoles - toxicity | Dogs | Protein Kinase Inhibitors - toxicity | Anti-Inflammatory Agents - chemical synthesis | Mice, Inbred BALB C | Protein Kinase Inhibitors - pharmacology | Heterocyclic Compounds, 2-Ring - chemical synthesis | Index Medicus | inhibition | amides | assays | peptides and proteins | hydrocarbons | 60 APPLIED LIFE SCIENCES
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6. Full Text Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: Optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches
by Huang, Boshi and Li, Cuicui and Chen, Wenmin and Liu, Tao and Yu, Mingyan and Fu, Lu and Sun, Yueyue and Liu, Huiqing and De Clercq, Erik and Pannecouque, Christophe and Balzarini, Jan and Zhan, Peng and Liu, Xinyong
European journal of medicinal chemistry, ISSN 0223-5234, 03/2015, Volume 92, pp. 754 - 765
Structure-based drug design | HIV-1 RT | Triazolopyrimidines | Biological activity | Physicochemical properties | Molecular simulations | Anti-HIV Agents - pharmacology | HIV Reverse Transcriptase - antagonists & inhibitors | Humans | Heterocyclic Compounds - pharmacology | Reverse Transcriptase Inhibitors - pharmacology | Heterocyclic Compounds - chemical synthesis | Structure-Activity Relationship | Sulfones - pharmacology | Anti-HIV Agents - chemical synthesis | Reverse Transcriptase Inhibitors - chemistry | Dose-Response Relationship, Drug | Microbial Sensitivity Tests | Reverse Transcriptase Inhibitors - chemical synthesis | Heterocyclic Compounds - chemistry | Sulfones - chemistry | Molecular Structure | Sulfones - chemical synthesis | HIV-1 - drug effects | Heterocyclic Compounds, 2-Ring - chemistry | Solubility | Models, Molecular | Heterocyclic Compounds, 2-Ring - pharmacology | HIV Reverse Transcriptase - metabolism | Anti-HIV Agents - chemistry | Nitrogen - chemistry | Cell Line, Tumor | Heterocyclic Compounds, 2-Ring - chemical synthesis | DNA polymerases | Antiviral agents | Pyrimidines | HIV (Viruses) | Analysis | Medical colleges | Index Medicus
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7. Full Text Synthesis of novel hetero ring fused pyridine derivatives; Their anticancer activity, CoMFA and CoMSIA studies
by Santhosh Kumar, G and Poornachandra, Y and Kumar Gunda, Shravan and Ratnakar Reddy, K and Mohmed, Jaheer and Shaik, Kamal and Ganesh Kumar, C and Narsaiah, B
Bioorganic & medicinal chemistry letters, ISSN 0960-894X, 07/2018, Volume 28, Issue 13, pp. 2328 - 2337
Carbohydrazide Schiff’s bases | 3D QSAR | CoMFA and CoMSIA studies | Anti-cancer activity | Pyrido[3′,2′:4,5]furo[3,2-d]pyrimidin-4(3H)-one | Carbohydrazide Schiff's bases | Heterocyclic Compounds, 3-Ring - pharmacology | Pyridines - chemistry | Pyrimidines - chemical synthesis | Antineoplastic Agents - chemical synthesis | Furans - pharmacology | Humans | Heterocyclic Compounds, 3-Ring - chemical synthesis | Pyrimidines - chemistry | Antineoplastic Agents - toxicity | Heterocyclic Compounds, 2-Ring - toxicity | Pyrimidines - toxicity | Furans - chemistry | HEK293 Cells | Heterocyclic Compounds, 3-Ring - toxicity | Antineoplastic Agents - pharmacology | Molecular Structure | Furans - toxicity | Quantitative Structure-Activity Relationship | Heterocyclic Compounds, 2-Ring - chemistry | Pyridines - chemical synthesis | Pyrimidines - pharmacology | Antineoplastic Agents - chemistry | Heterocyclic Compounds, 2-Ring - pharmacology | Cyclization | Hydrogen Bonding | Pyridines - toxicity | Heterocyclic Compounds, 3-Ring - chemistry | Cell Line, Tumor | Pyridines - pharmacology | Furans - chemical synthesis | Heterocyclic Compounds, 2-Ring - chemical synthesis | Drug Screening Assays, Antitumor | Alkaloids | Amines | Pyridine | Aldehydes | Analysis | Index Medicus
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8. Full Text Design, synthesis and biological evaluation of novel dual-acting modulators targeting both estrogen receptor α (ERα) and lysine-specific demethylase 1 (LSD1) for treatment of breast cancer
by He, Ming and Ning, Wentao and Hu, Zhiye and Huang, Jian and Dong, Chune and Zhou, Hai-Bing
European journal of medicinal chemistry, ISSN 0223-5234, 06/2020, Volume 195, pp. 112281 - 112281
Estrogen receptor | OBHS-LSD1i conjugates | Breast cancer | Lysine specific demethylase 1 | Selective estrogen receptor modulators | Cell Survival - drug effects | Chemistry Techniques, Synthetic | Estrogen Receptor alpha - chemistry | Antineoplastic Agents - chemical synthesis | Humans | Heterocyclic Compounds, 2-Ring - chemistry | Models, Molecular | Antineoplastic Agents - therapeutic use | Antineoplastic Agents - chemistry | Molecular Targeted Therapy | Heterocyclic Compounds, 2-Ring - pharmacology | Histone Demethylases - metabolism | MCF-7 Cells | Breast Neoplasms - pathology | Heterocyclic Compounds, 2-Ring - therapeutic use | Drug Design | Estrogen Receptor alpha - metabolism | Protein Conformation | Antineoplastic Agents - pharmacology | Heterocyclic Compounds, 2-Ring - chemical synthesis | Index Medicus
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9. Full Text Discovery of the Soluble Guanylate Cyclase Stimulator Vericiguat (BAY 1021189) for the Treatment of Chronic Heart Failure
by Follmann, Markus and Ackerstaff, Jens and Redlich, Gorden and Wunder, Frank and Lang, Dieter and Kern, Armin and Fey, Peter and Griebenow, Nils and Kroh, Walter and Becker-Pelster, Eva-Maria and Kretschmer, Axel and Geiss, Volker and Li, Volkhart and Straub, Alexander and Mittendorf, Joachim and Jautelat, Rolf and Schirok, Hartmut and Schlemmer, Karl-Heinz and Lustig, Klemens and Gerisch, Michael and Knorr, Andreas and Tinel, Hanna and Mondritzki, Thomas and Trübel, Hubert and Sandner, Peter and Stasch, Johannes-Peter
Journal of medicinal chemistry, ISSN 0022-2623, 06/2017, Volume 60, Issue 12, pp. 5146 - 5161
Chemistry Techniques, Synthetic | Rats, Transgenic | Rats, Wistar | Soluble Guanylyl Cyclase - metabolism | Administration, Oral | Pyrimidines - administration & dosage | Humans | Heterocyclic Compounds, 2-Ring - administration & dosage | Heterocyclic Compounds, 2-Ring - chemistry | Male | NG-Nitroarginine Methyl Ester - adverse effects | Structure-Activity Relationship | Pyrimidines - pharmacology | Pyrimidines - chemistry | Heart Failure - drug therapy | Heterocyclic Compounds, 2-Ring - pharmacology | Administration, Intravenous | Animals | Soluble Guanylyl Cyclase - genetics | Dogs | Blood Pressure - drug effects | Hepatocytes - drug effects | Index Medicus
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10. Omarigliptin: First Global Approval
by Burness, Celeste B
Drugs (New York, N.Y.), ISSN 0012-6667, 11/2015, Volume 75, Issue 16, pp. 1947 - 1952
Pharmacology & Pharmacy | Toxicology | Life Sciences & Biomedicine | Science & Technology | Hypoglycemic Agents - therapeutic use | Dipeptidyl-Peptidase IV Inhibitors - adverse effects | Dipeptidyl-Peptidase IV Inhibitors - therapeutic use | Humans | Drug Approval | Heterocyclic Compounds, 2-Ring - pharmacokinetics | Dipeptidyl-Peptidase IV Inhibitors - pharmacology | Heterocyclic Compounds, 2-Ring - pharmacology | Heterocyclic Compounds, 2-Ring - adverse effects | Pyrans - pharmacokinetics | Dipeptidyl-Peptidase IV Inhibitors - pharmacokinetics | Heterocyclic Compounds, 2-Ring - therapeutic use | Internationality | Pyrans - adverse effects | Diabetes Mellitus, Type 2 - drug therapy | Drug Therapy, Combination | Pyrans - pharmacology | Pyrans - therapeutic use
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11. Full Text Optimization of a Series of Bivalent Triazolopyridazine Based Bromodomain and Extraterminal Inhibitors: The Discovery of (3R)‑4-[2-[4-[1-(3-Methoxy-[1,2,4]triazolo[4,3‑b]pyridazin-6-yl)-4-piperidyl]phenoxy]ethyl]-1,3-dimethyl-piperazin-2-one (AZD5153)
by Bradbury, Robert H and Callis, Rowena and Carr, Gregory R and Chen, Huawei and Clark, Edwin and Feron, Lyman and Glossop, Steve and Graham, Mark A and Hattersley, Maureen and Jones, Chris and Lamont, Scott G and Ouvry, Gilles and Patel, Anil and Patel, Joe and Rabow, Alfred A and Roberts, Craig A and Stokes, Stephen and Stratton, Natalie and Walker, Graeme E and Ward, Lara and Whalley, David and Whittaker, David and Wrigley, Gail and Waring, Michael J
Journal of medicinal chemistry, ISSN 0022-2623, 09/2016, Volume 59, Issue 17, pp. 7801 - 7817
Neoplasm Transplantation | Stereoisomerism | Humans | Crystallography, X-Ray | Piperazines - chemistry | Structure-Activity Relationship | Hepatocytes - metabolism | Heterografts | Female | Antineoplastic Agents - pharmacokinetics | Antineoplastic Agents - pharmacology | Piperazines - pharmacokinetics | Hepatocytes - drug effects | Caco-2 Cells | Heterocyclic Compounds, 2-Ring - chemistry | Rats | Transcription Factors - antagonists & inhibitors | Heterocyclic Compounds, 2-Ring - pharmacokinetics | Antineoplastic Agents - chemistry | Mice, SCID | Piperazines - pharmacology | Heterocyclic Compounds, 2-Ring - pharmacology | Animals | Nuclear Proteins - antagonists & inhibitors | Dogs | Protein Conformation | Index Medicus
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12. Full Text Optimization of Fused Bicyclic Allosteric SHP2 Inhibitors
by Bagdanoff, Jeffrey T and Chen, Zhouliang and Acker, Michael and Chen, Ying-Nan and Chan, Homan and Dore, Michael and Firestone, Brant and Fodor, Michelle and Fortanet, Jorge and Hentemann, Murphy and Kato, Mitsunori and Koenig, Robert and LaBonte, Laura R and Liu, Shumei and Mohseni, Movarid and Ntaganda, Rukundo and Sarver, Patrick and Smith, Troy and Sendzik, Martin and Stams, Travis and Spence, Stan and Towler, Christopher and Wang, Hongyun and Wang, Ping and Williams, Sarah L and LaMarche, Matthew J and Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Journal of medicinal chemistry, ISSN 0022-2623, 02/2019, Volume 62, Issue 4, pp. 1781 - 1792
Protein Tyrosine Phosphatase, Non-Receptor Type 11 - metabolism | Pyrazoles - chemical synthesis | Allosteric Regulation | Humans | Microsomes, Liver - metabolism | Male | Structure-Activity Relationship | Pyrimidinones - metabolism | Enzyme Inhibitors - chemical synthesis | Pyrimidinones - pharmacology | Molecular Structure | Pyrimidinones - chemical synthesis | Pyrazoles - pharmacology | Enzyme Inhibitors - metabolism | Mice, Inbred C57BL | Enzyme Inhibitors - pharmacology | Protein Tyrosine Phosphatase, Non-Receptor Type 11 - antagonists & inhibitors | Protein Tyrosine Phosphatase, Non-Receptor Type 11 - chemistry | Pyrazoles - metabolism | Rats, Sprague-Dawley | Heterocyclic Compounds, 2-Ring - pharmacology | Animals | MAP Kinase Signaling System - drug effects | Heterocyclic Compounds, 2-Ring - metabolism | Allosteric Site | Cell Line, Tumor | Protein Binding | Molecular Docking Simulation | Heterocyclic Compounds, 2-Ring - chemical synthesis | Index Medicus | Peptides and proteins | Selectivity | INORGANIC, ORGANIC, PHYSICAL, AND ANALYTICAL CHEMISTRY | Amines | Inhibitors | Rodent models
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13. Full Text RAF inhibitors that evade paradoxical MAPK pathway activation
by Zhang, Chao and Spevak, Wayne and Zhang, Ying and Burton, Elizabeth A and Ma, Yan and Habets, Gaston and Zhang, Jiazhong and Lin, Jack and Ewing, Todd and Matusow, Bernice and Tsang, Garson and Marimuthu, Adhirai and Cho, Hanna and Wu, Guoxian and Wang, Weiru and Fong, Daniel and Nguyen, Hoa and Shi, Songyuan and Womack, Patrick and Nespi, Marika and Shellooe, Rafe and Carias, Heidi and Powell, Ben and Light, Emily and Sanftner, Laura and Walters, Jason and Tsai, James and West, Brian L and Visor, Gary and Rezaei, Hamid and Lin, Paul S and Nolop, Keith and Ibrahim, Prabha N and Hirth, Peter and Bollag, Gideon
Nature (London), ISSN 0028-0836, 10/2015, Volume 526, Issue 7574, pp. 583 - 586
Science & Technology - Other Topics | Multidisciplinary Sciences | Science & Technology | Humans | Protein Kinase Inhibitors - adverse effects | Enzyme Activation - drug effects | Mutation - genetics | Sulfonamides - pharmacology | Heterocyclic Compounds, 2-Ring - pharmacology | Heterocyclic Compounds, 2-Ring - adverse effects | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Animals | Indoles - adverse effects | MAP Kinase Signaling System - drug effects | MAP Kinase Signaling System - genetics | Models, Biological | Proto-Oncogene Proteins B-raf - genetics | Cell Line, Tumor | Sulfonamides - adverse effects | Female | Indoles - pharmacology | Mice | Protein Kinase Inhibitors - pharmacology | Genes, ras - genetics | Mitogen-Activated Protein Kinases - metabolism | Genetic aspects | Metastasis | Gene mutations | Observations | Health aspects | Mitogen-activated protein kinases | Epidermal growth factor | Melanoma | Ligands | Kinases | Gene expression | Tumors | Crystal structure | Index Medicus
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14. Full Text Structure−Activity Relationship of New Anti-Hepatitis C Virus Agents: Heterobicycle−Coumarin Conjugates
by Neyts, Johan and Clercq, Erik De and Singha, Raghunath and Chang, Yung Hsiung and Das, Asish R and Chakraborty, Subhasish K and Hong, Shih Ching and Tsay, Shwu-Chen and Hsu, Ming-Hua and Hwu, Jih Ru
Journal of medicinal chemistry, ISSN 0022-2623, 03/2009, Volume 52, Issue 5, pp. 1486 - 1490
Antiviral agents | Biological and medical sciences | Medical sciences | Pharmacology. Drug treatments | Antibiotics. Antiinfectious agents. Antiparasitic agents | Benzoxazoles - pharmacology | Pyridines - chemistry | Humans | Imidazoles - chemistry | Hepacivirus - genetics | Coumarins - chemistry | Structure-Activity Relationship | Antiviral Agents - chemistry | Imidazoles - chemical synthesis | Hepacivirus - drug effects | Purines - chemical synthesis | Cell Line | Virus Replication - drug effects | Antiviral Agents - pharmacology | Purines - pharmacology | Heterocyclic Compounds, 2-Ring - chemistry | Pyridines - chemical synthesis | Models, Molecular | Imidazoles - pharmacology | Benzoxazoles - chemical synthesis | Heterocyclic Compounds, 2-Ring - pharmacology | Coumarins - pharmacology | Benzoxazoles - chemistry | Purines - chemistry | Coumarins - chemical synthesis | Antiviral Agents - chemical synthesis | Cell Proliferation - drug effects | Pyridines - pharmacology | RNA, Viral - drug effects | Heterocyclic Compounds, 2-Ring - chemical synthesis | Index Medicus
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15. Full Text Hippocampal Sirtuin 1 Signaling Mediates Depression-like Behavior
by Abe-Higuchi, Naoko and Uchida, Shusaku and Yamagata, Hirotaka and Higuchi, Fumihiro and Hobara, Teruyuki and Hara, Kumiko and Kobayashi, Ayumi and Watanabe, Yoshifumi
Biological psychiatry (1969), ISSN 0006-3223, 12/2016, Volume 80, Issue 11, pp. 815 - 826
Dendritic atrophy | Depression | Chronic stress | Anxiety | Sirtuin | Hippocampus | Neurosciences | Neurosciences & Neurology | Life Sciences & Biomedicine | Psychiatry | Science & Technology | Sirtuin 1 - metabolism | Dendrites - pathology | Stilbenes - administration & dosage | Male | Stilbenes - pharmacology | Imipramine - administration & dosage | Enzyme Inhibitors - administration & dosage | Benzamides - administration & dosage | Depression - metabolism | Stress, Psychological - metabolism | Naphthols - administration & dosage | Benzamides - pharmacology | Antidepressive Agents, Tricyclic - administration & dosage | Disease Models, Animal | Dentate Gyrus - metabolism | Mice, Inbred C57BL | Naphthols - pharmacology | Enzyme Inhibitors - pharmacology | Heterocyclic Compounds, 2-Ring - administration & dosage | Sirtuin 1 - antagonists & inhibitors | Heterocyclic Compounds, 2-Ring - pharmacology | Hippocampus - metabolism | Animals | Antidepressive Agents, Tricyclic - pharmacology | Signal Transduction - physiology | Mice | Mice, Inbred BALB C | Imipramine - pharmacology | Stress (Psychology) | Depression, Mental | Protein kinases | Analysis | Index Medicus
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16. Full Text Thiol-Based Probe for Electrophilic Natural Products Reveals That Most of the Ammosamides Are Artifacts
by Reimer, Daniela and Hughes, Chambers C
Journal of natural products (Washington, D.C.), ISSN 0163-3864, 01/2017, Volume 80, Issue 1, pp. 126 - 133
Amides - pharmacology | Sulfhydryl Compounds - pharmacology | Heterocyclic Compounds, 3-Ring - pharmacology | Humans | Quinolines - chemistry | Heterocyclic Compounds, 2-Ring - chemistry | Biological Products - pharmacology | Biological Products - isolation & purification | Quinolines - pharmacology | Heterocyclic Compounds, 2-Ring - pharmacology | Amides - isolation & purification | Biological Products - chemistry | Heterocyclic Compounds, 3-Ring - isolation & purification | Heterocyclic Compounds, 3-Ring - chemistry | Amides - chemistry | Heterocyclic Compounds, 2-Ring - isolation & purification | Sulfhydryl Compounds - chemistry | Molecular Structure | Streptomyces - drug effects | Quinolines - isolation & purification | Index Medicus
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17. Full Text Synthesis, antitumor evaluation and molecular docking studies of [1,2,4]triazolo[4,3-b][1,2,4,5]tetrazine derivatives
by Xu, Feng and Yang, Zhen-zhen and Jiang, Jun-rong and Pan, Wan-gui and Yang, Xiao-le and Wu, Jian-yong and Zhu, Yan and Wang, John and Shou, Qi-Yang and Wu, Han-gui
Bioorganic & medicinal chemistry letters, ISSN 0960-894X, 07/2016, Volume 26, Issue 13, pp. 3042 - 3047
X-ray diffraction | Antitumor activity | Triazole | Docking study | Toxicity | Tetrazine | Triazoles - administration & dosage | Proto-Oncogene Proteins c-met - antagonists & inhibitors | Antineoplastic Agents - chemical synthesis | Humans | Heterocyclic Compounds, 2-Ring - administration & dosage | Structure-Activity Relationship | Antineoplastic Agents - administration & dosage | Mice, Inbred ICR | Antineoplastic Agents - toxicity | Heterocyclic Compounds, 2-Ring - pharmacology | Triazoles - pharmacology | Heterocyclic Compounds, 2-Ring - toxicity | Animals | Triazoles - toxicity | MCF-7 Cells | HL-60 Cells | Inhibitory Concentration 50 | Triazoles - chemical synthesis | Antineoplastic Agents - pharmacology | Molecular Docking Simulation | Binding Sites | Heterocyclic Compounds, 2-Ring - chemical synthesis | Staurosporine - pharmacology | Drug Screening Assays, Antitumor | Index Medicus
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