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1. Full Text MCR synthesis of a tetracyclic tetrazole scaffold
by Patil, Pravin and Khoury, Kareem and Herdtweck, Eberhardt and Dömling, Alexander
Bioorganic & medicinal chemistry, ISSN 0968-0896, 06/2015, Volume 23, Issue 11, pp. 2699 - 2715
Synthesis | Tetrazol | Parallel | Isocyanide | Ugi | Pictet–Spengler | unclassified drug | n [[(4 chlorophenyl)[1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl]methyl] 2 3,4 dimethoxyphenyl]ethanamine | 8 ethyl 2,3 dimethoxy 8 methyl 6,8,13,13a tetrahydro 5h tetrazolo[1',5' 4,5]pyrazino [2,1 a]isoquinoline | n [2 (1h indol 3 yl)ethyl] 1 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl]propan 1 amine | tetracyclic tetrazole scaffold | 1 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl] n (3,4 dimethoxyphenethyl)cyclohexanamine | n [[1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl](4 fluorophenyl)methyl] 2 (3,4 dimethoxy phenyl)ethanamine | 8 (4 chlorophenyl) 2,3 dimethoxy 6,8,13,13a tetrahydro 5h tetrazolo[1',5' 4,5]pyrazino [2,1 a]isoquinoline | 8 isopropyl 2,3 dimethoxy 6,8,13,13a tetrahydro 5h tetrazoleo[1',5' 4,5]pyrazino [2,1 a]isoquinoline | 1 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl] n (3,4 dimethoxyphenethyl) 2 phenylethanamine | high throughput screening | mass spectrometry | Pictet-Spengler | multicomponent reaction chemistry | 1 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl] n (3,4 dimethoxyphenethyl)propan 1 amine | thin layer chromatography | 1 benzyl 4 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl] n (3,4 dimethoxy phenethyl)piperidin 4 amine | proton nuclear magnetic resonance | n [2 (1h indol 3 yl)ethyl] 1 benzyl 4 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl]piperidin 4 amine | 2,3 dimethoxy 8 phenyl 6,8,13,13a tetrahydro 5h tetrazolo[1',5' 4,5]pyrazino [2,1 a]isoquinoline | 7',12',12b',13' tetrahydro 6'h spiro[cyclohexane 1,4' tetrazolo[1'',5'' 4',5']pyrazino[1',2' 1,2]pyrido[3,4 b]indole] | 1 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl] n (3,4 dimethoxyphenethyl) 2 phenylpropan 1 amine | 2,3 dimethoxy 8 phenethyl 6,8,13,13a tetrahydro 5h tetrazoleo[1',5' 4,5]pyrazino [2,1 a]isoquinoline | chemical reaction | supercritical fluid chromatography | tetrazole derivative | n [2 (1h indol 3 yl)ethyl] 1 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl]cyclohexanamine | article | carbon nuclear magnetic resonance | n [[1,1' biphenyl] 4 yl[1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl]methyl] 2 (3,4 dimethoxyphenyl)ethanamine | controlled study | 8 (4 fluorophenyl) 2,3 dimethoxy 6,8,13,13a tetrahydro 5h tetrazolo[1',5' 4,5]pyrazino [2,1 a]isoquinoline | 8 benzyl 2,3 dimethoxy 6,8,13,13a tetrahydro 5h tetrazoleo[1',5' 4,5]pyrazino [2,1 a]isoquinoline | 8 ethyl 2,3 dimethoxy 6,8,13,13a tetrahydro 5h tetrazoleo[1',5' 4,5]pyrazino [2,1 a]isoquinoline | 1 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl] n (3,4 dimethoxyphenethyl) 2 methylpropan 1 amine | 8 [[1,1' biphenyl] 4 yl] 2,3 dimethoxy 6,8,13,13a tetrahydro 5h tetrazolo[1',5' 4,5]pyrazino [2,1 a]isoquinoline | 1 benzyl 2',3'dimethoxy 5',6',13',13a' tetrahydrospiro[piperidine 4,8' tetrazolo[1',5' 4,5]pyrazino [2,1 a]isoquinoline] | 4 ethyl 4,6,7,12,12b,13 hexahydro tetrazolo[1'',5'' 4',5']pyrazino[1',2' 1,2]pyrido[3,4 b]indole | 2',3'dimethoxy 5',6',13',13a' tetrahydrospiro[cyclohexane 1,8' tetrazolo[1',5' 4,5]pyrazino [2,1 a]isoquinoline] | unindexed drug | pharmacophore | n [[1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl](phenyl)methyl] 2 (3,4 dimethoxy phenyl)ethanamine | 2 [1 (2,2 dimethoxyethyl) 1h tetrazole 5 yl] n (3,4 dimethoxyphenethyl)butan 2 amine | Models, Molecular | Molecular Structure | Tetrazoles - chemical synthesis | Polycyclic Compounds - chemical synthesis | Drug Discovery | Index Medicus | Pictet-spengler
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2. Full Text 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)
by Kung, Pei-Pei and Bingham, Patrick and Brooun, Alexei and Collins, Michael and Deng, Ya-Li and Dinh, Dac and Fan, Connie and Gajiwala, Ketan S and Grantner, Rita and Gukasyan, Hovhannes J and Hu, Wenyue and Huang, Buwen and Kania, Robert and Kephart, Susan E and Krivacic, Cody and Kumpf, Robert A and Khamphavong, Penney and Kraus, Manfred and Liu, Wei and Maegley, Karen A and Nguyen, Lisa and Ren, Shijian and Richter, Dan and Rollins, Robert A and Sach, Neal and Sharma, Shikhar and Sherrill, John and Spangler, Jillian and Stewart, Albert E and Sutton, Scott and Uryu, Sean and Verhelle, Dominique and Wang, Hui and Wang, Shuiwang and Wythes, Martin and Xin, Shuibo and Yamazaki, Shinji and Zhu, Huichun and Zhu, Jinjiang and Zehnder, Luke and Edwards, Martin
Journal of medicinal chemistry, ISSN 0022-2623, 02/2018, Volume 61, Issue 3, pp. 650 - 665
Enhancer of Zeste Homolog 2 Protein - antagonists & inhibitors | Isoquinolines - chemistry | Isoquinolines - pharmacology | Isoquinolines - pharmacokinetics | Administration, Oral | Humans | Molecular Conformation | Drug Design | Cell Line, Tumor | Models, Molecular | Biological Availability | Isoquinolines - administration & dosage | Index Medicus
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3. Full Text Daclatasvir plus asunaprevir for chronic HCV genotype 1b infection
by Kumada, Hiromitsu and Suzuki, Yoshiyuki and Ikeda, Kenji and Toyota, Joji and Karino, Yoshiyasu and Chayama, Kazuaki and Kawakami, Yoshiiku and Ido, Akio and Yamamoto, Kazuhide and Takaguchi, Koichi and Izumi, Namiki and Koike, Kazuhiko and Takehara, Tetsuo and Kawada, Norifumi and Sata, Michio and Miyagoshi, Hidetaka and Eley, Timothy and McPhee, Fiona and Damokosh, Andrew and Ishikawa, Hiroki and Hughes, Eric
Hepatology (Baltimore, Md.), ISSN 0270-9139, 06/2014, Volume 59, Issue 6, pp. 2083 - 2091
Gastroenterology & Hepatology | Life Sciences & Biomedicine | Science & Technology | Isoquinolines - adverse effects | Humans | Imidazoles - adverse effects | Middle Aged | Hepacivirus - genetics | Hepatitis C, Chronic - virology | Male | RNA, Viral - blood | Isoquinolines - blood | Hepatitis C, Chronic - drug therapy | Hepatitis C, Chronic - blood | Young Adult | Imidazoles - blood | Sulfonamides - blood | Sulfonamides - therapeutic use | Treatment Failure | Isoquinolines - therapeutic use | Sulfonamides - adverse effects | Adult | Female | Aged | Imidazoles - therapeutic use | Drug Therapy, Combination | Genotype & phenotype | Interferon | Infections | Drug therapy | Hepatology | Index Medicus | Rapid Communication
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4. Full Text Ruthenium-Catalyzed C–H/N–O Bond Functionalization: Green Isoquinolone Syntheses in Water
by Ackermann, Lutz and Fenner, Sabine
Organic letters, ISSN 1523-7060, 12/2011, Volume 13, Issue 24, pp. 6548 - 6551
Isoquinolines - chemistry | Carboxylic Acids - chemistry | Isoquinolines - chemical synthesis | Water - chemistry | Alkynes - chemistry | Colorimetry | Molecular Structure | Catalysis | Ruthenium - chemistry | Benzamides - chemistry | Index Medicus
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5. Full Text Discovery and Optimization of Isoquinoline Ethyl Ureas as Antibacterial Agents
by Panchaud, Philippe and Bruyère, Thierry and Blumstein, Anne-Catherine and Bur, Daniel and Chambovey, Alain and Ertel, Eric A and Gude, Markus and Hubschwerlen, Christian and Jacob, Loïc and Kimmerlin, Thierry and Pfeifer, Thomas and Prade, Lars and Seiler, Peter and Ritz, Daniel and Rueedi, Georg
Journal of medicinal chemistry, ISSN 0022-2623, 05/2017, Volume 60, Issue 9, pp. 3755 - 3775
Isoquinolines - pharmacokinetics | Area Under Curve | Solubility | Half-Life | Rats | Respiratory Tract Infections - drug therapy | Potassium Channels - drug effects | Drug Discovery | Urea - chemistry | Microbial Sensitivity Tests | Respiratory Tract Infections - microbiology | Gram-Negative Bacteria - drug effects | Isoquinolines - chemistry | Animals | Isoquinolines - pharmacology | Hydrogen Bonding | Anti-Bacterial Agents - chemistry | Isoquinolines - therapeutic use | Anti-Bacterial Agents - pharmacology | Index Medicus
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6. Full Text Phase II Study of ET-743 in Advanced Soft Tissue Sarcomas: A European Organisation for the Research and Treatment of Cancer (EORTC) Soft Tissue and Bone Sarcoma Group Trial
by A. Le Cesne and J.Y. Blay and I. Judson and A. Van Oosterom and J. Verweij and J. Radford and P. Lorigan and S. Rodenhuis and I. Ray-Coquard and S. Bonvalot and F. Collin and J. Jimeno and E. Di Paola and M. Van Glabbeke and O.S. Nielsen
Journal of clinical oncology, ISSN 0732-183X, 01/2005, Volume 23, Issue 3, pp. 576 - 584
Life Sciences & Biomedicine | Oncology | Science & Technology | Tumors of the skin and soft tissue. Premalignant lesions | Biological and medical sciences | Medical sciences | Dermatology | Tumors | Dioxoles - therapeutic use | Isoquinolines - adverse effects | Dioxoles - adverse effects | Humans | Middle Aged | Antineoplastic Agents, Alkylating - pharmacology | Male | Antineoplastic Agents, Alkylating - administration & dosage | Isoquinolines - pharmacology | Dioxoles - administration & dosage | Aged, 80 and over | Dioxoles - pharmacology | Adult | Female | Tetrahydroisoquinolines | Drug Administration Schedule | Treatment Outcome | Sarcoma - drug therapy | Disease Progression | Antineoplastic Agents, Alkylating - therapeutic use | Disease-Free Survival | Adolescent | Isoquinolines - therapeutic use | Aged | Infusions, Intravenous | Antineoplastic Agents, Alkylating - adverse effects | Isoquinolines - administration & dosage | Index Medicus
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7. Full Text A selective inhibitor of PRMT5 with in vivo and in vitro potency in MCL models
by Chan-Penebre, Elayne and Kuplast, Kristy G and Majer, Christina R and Boriack-Sjodin, P Ann and Wigle, Tim J and Johnston, L Danielle and Rioux, Nathalie and Munchhof, Michael J and Jin, Lei and Jacques, Suzanne L and West, Kip A and Lingaraj, Trupti and Stickland, Kimberly and Ribich, Scott A and Raimondi, Alejandra and Scott, Margaret Porter and Waters, Nigel J and Pollock, Roy M and Smith, Jesse J and Barbash, Olena and Pappalardi, Melissa and Ho, Thau F and Nurse, Kelvin and Oza, Khyati P and Gallagher, Kathleen T and Kruger, Ryan and Moyer, Mikel P and Copeland, Robert A and Chesworth, Richard and Duncan, Kenneth W and Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Nature chemical biology, ISSN 1552-4450, 06/2015, Volume 11, Issue 6, pp. 432 - 437
Life Sciences & Biomedicine | Biochemistry & Molecular Biology | Science & Technology | Humans | Lymphoma, Mantle-Cell - pathology | Protein-Arginine N-Methyltransferases - antagonists & inhibitors | Crystallography, X-Ray | Male | Antineoplastic Agents - therapeutic use | snRNP Core Proteins - metabolism | Pyrimidines - chemistry | Dose-Response Relationship, Drug | Isoquinolines - chemistry | Isoquinolines - pharmacology | Inhibitory Concentration 50 | Antineoplastic Agents - pharmacology | Molecular Structure | Cell Death - drug effects | Lymphoma, Mantle-Cell - drug therapy | Models, Molecular | Pyrimidines - pharmacology | Antineoplastic Agents - chemistry | Mice, Inbred Strains | Xenograft Model Antitumor Assays | Animals | Lymphoma, Mantle-Cell - enzymology | Pyrimidines - therapeutic use | Cell Line, Tumor | Isoquinolines - therapeutic use | Protein Binding | Cell Proliferation - drug effects | Methylation | Proteins | Biochemistry | Cellular biology | Colorectal cancer | Index Medicus
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8. Full Text Synthesis of Isoquinolines via Rh(III)-Catalyzed C–H Activation Using Hydrazone as a New Oxidizing Directing Group
by Chuang, Sheng-Chieh and Gandeepan, Parthasarathy and Cheng, Chien-Hong
Organic letters, ISSN 1523-7060, 11/2013, Volume 15, Issue 22, pp. 5750 - 5753
Isoquinolines - chemistry | Hydrogen Bonding | Isoquinolines - chemical synthesis | Molecular Structure | Catalysis | Hydrazones - chemistry | Rhodium - chemistry | Index Medicus
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9. Full Text Duvelisib, a novel oral dual inhibitor of PI3K-delta,gamma, is clinically active in advanced hematologic malignancies
by Flinn, Ian W and O'Brien, Susan and Kahl, Brad and Patel, Manish and Oki, Yasuhiro and Foss, Francine F and Porcu, Pierluigi and Jones, Jeffrey and Burger, Jan A and Jain, Nitin and Kelly, Virginia M and Allen, Kerstin and Douglas, Mark and Sweeney, Jennifer and Kelly, Patrick and Horwitz, Steven
Blood, ISSN 0006-4971, 02/2018, Volume 131, Issue 8, pp. 877 - 887
Life Sciences & Biomedicine | Hematology | Science & Technology | Phosphoinositide-3 Kinase Inhibitors | Prognosis | Isoquinolines - pharmacokinetics | Administration, Oral | Purines - pharmacology | Humans | Middle Aged | Purines - pharmacokinetics | Male | Hematologic Neoplasms - enzymology | Hematologic Neoplasms - pathology | Purines - administration & dosage | Class I Phosphatidylinositol 3-Kinases - antagonists & inhibitors | Tissue Distribution | Maximum Tolerated Dose | Isoquinolines - pharmacology | Aged, 80 and over | Class Ib Phosphatidylinositol 3-Kinase | Hematologic Neoplasms - drug therapy | Adult | Female | Aged | Safety | Isoquinolines - administration & dosage | Index Medicus | Abridged Index Medicus | Lymphoid Neoplasia
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10. Full Text A Structure–Activity Analysis of Biased Agonism at the Dopamine D2 Receptor
by Shonberg, Jeremy and Herenbrink, Carmen Klein and López, Laura and Christopoulos, Arthur and Scammells, Peter J and Capuano, Ben and Lane, J. Robert
Journal of medicinal chemistry, ISSN 0022-2623, 11/2013, Volume 56, Issue 22, pp. 9199 - 9221
Isoquinolines - metabolism | Cricetinae | Cricetulus | Stereoisomerism | Humans | Receptors, Dopamine D2 - agonists | Structure-Activity Relationship | Receptors, Dopamine D2 - metabolism | Dose-Response Relationship, Drug | Isoquinolines - chemistry | Animals | Isoquinolines - pharmacology | Isoquinolines - chemical synthesis | Receptors, Dopamine D2 - chemistry | Protein Conformation | Molecular Docking Simulation | CHO Cells | Index Medicus
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11. Full Text 3-Arylisoquinolines as novel topoisomerase I inhibitors
by Khadka, Daulat Bikram and Cho, Won-Jea
Bioorganic & medicinal chemistry, ISSN 0968-0896, 2011, Volume 19, Issue 2, pp. 724 - 734
Indeno[1,2- c]isoquinoline | Camptothecin | Benz[ b]oxepine | 3-Arylisoquinoline | Isoindolo[2,1- b]isoquinoline | 12-Oxobenzo[ c]phenanthridine | Topoisomerase I inhibitor | Isoindolo[2,1-b]isoquinoline | 12-Oxobenzo[c]phenanthridine | Benz[b]oxepine | Indeno[1,2-c]isoquinoline | Biochemistry & Molecular Biology | Physical Sciences | Chemistry | Chemistry, Organic | Life Sciences & Biomedicine | Pharmacology & Pharmacy | Chemistry, Medicinal | Science & Technology | Biological and medical sciences | General aspects | Medical sciences | Antineoplastic agents | Pharmacology. Drug treatments | Isoquinolines - chemistry | Topoisomerase I Inhibitors - chemical synthesis | DNA Topoisomerases, Type I - metabolism | Antineoplastic Agents - chemical synthesis | Isoquinolines - chemical synthesis | DNA Topoisomerases, Type I - chemistry | Antineoplastic Agents - chemistry | Topoisomerase I Inhibitors - toxicity | Isoquinolines - toxicity | Topoisomerase I Inhibitors - chemistry | Antineoplastic Agents - toxicity | Index Medicus | Alkaloids
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12. Full Text Discovery and development of orexin receptor antagonists as therapeutics for insomnia
by Winrow, C J and Renger, J J
British journal of pharmacology, ISSN 0007-1188, 01/2014, Volume 171, Issue 2, pp. 283 - 293
sleep | GABA | orexin receptor antagonist | insomnia | Life Sciences & Biomedicine | Pharmacology & Pharmacy | Science & Technology | Orexin Receptor Antagonists | Isoquinolines - adverse effects | Acetamides - pharmacokinetics | Hypnotics and Sedatives - adverse effects | Hypnotics and Sedatives - pharmacokinetics | Isoquinolines - pharmacokinetics | Orexins | Humans | Acetamides - pharmacology | Biological Availability | Hypnotics and Sedatives - therapeutic use | Neuropeptides - physiology | Animals | High-Throughput Screening Assays | Isoquinolines - pharmacology | Acetamides - therapeutic use | Signal Transduction - drug effects | Drug Design | Acetamides - adverse effects | Isoquinolines - therapeutic use | Hypnotics and Sedatives - pharmacology | Intracellular Signaling Peptides and Proteins - physiology | Sleep Initiation and Maintenance Disorders - drug therapy | Insomnia | Analysis | Sleep | Drug therapy | Digestive system | Index Medicus | Themed Section | Orexin Receptors
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13. Full Text Cp∗CoIII Catalyzed Site-Selective C-H Activation of Unsymmetrical O-Acyl Oximes: Synthesis of Multisubstituted Isoquinolines from Terminal and Internal Alkynes
by Sun, Bo and Yoshino, Tatsuhiko and Kanai, Motomu and Matsunaga, Shigeki
Angewandte Chemie (International ed.), ISSN 1433-7851, 10/2015, Volume 54, Issue 44, pp. 12968 - 12972
isoquinolines | C-H activation | transition-metal catalysis | cobalt
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