Page last updated: 2024-08-21

pyrazines and indazoles

pyrazines has been researched along with indazoles in 36 studies

Research

Studies (36)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's0 (0.00)29.6817
2010's25 (69.44)24.3611
2020's11 (30.56)2.80

Authors

AuthorsStudies
Kocí, J; Krchnák, V; Oliver, AG1
Brown, KK; Choudhry, AE; Heerding, DA; Kumar, R; Lai, Z; Lin, H; Luengo, JI; Minthorn, EA; Rhodes, N; Robell, KA; Verma, S; Xie, R; Yamashita, DS; Zeng, J; Zhang, S1
Arango, BA; Cohen, EE; Perez, CA; Raez, LE; Santos, ES1
Fuchi, N; Fujii, S; Iura, Y; Kaneko, H; Nishimura, K; Nitta, A; Sekiya, Y; Suyama, K; Takahashi, T; Ueda, H; Yamada, M; Yamaguchi, S1
Aiello, R; Aspnes, GE; Atkinson, K; Baker, L; Barucci, N; Bian, J; Bourassa, P; Bourbonais, F; Bourbounais, F; D'Aquila, T; Derksen, DR; Filipski, KJ; Guzman-Perez, A; Hamilton, M; Hank, R; Jones, CS; Karki, K; Li, JC; Litchfield, J; MacDougall, M; Patel, L; Pfefferkorn, JA; Rasmusson, T; Robertson, A; Sammons, MF; Song, W; Tu, M; Zeng, D1
DeVicente, J; Hermann, JC; Jaime-Figueroa, S; Jin, S; Kuglstatter, A; Li, H; Lovey, A; Lynch, SM; Menke, J; Niu, L; Patel, V; Roy, D; Soth, M; Steiner, S; Tivitmahaisoon, P; Vu, MD; Yee, C1
Burke, RT; Clarke, AS; Currie, KS; Dipaolo, JA; Druker, BJ; Lannutti, BJ; Loriaux, MM; Maciejewski, P; Meadows, S; Mitchell, SA; Spurgeon, SE1
Barbosa, J; Blomgren, P; Currie, KS; Di Paolo, JA; Gallion, S; Kropf, JE; Lansdon, EB; Lee, T; Macaluso, J; Maciejewski, P; Maclin, D; Mitchell, SA; Rong, H; Rossi, AM; Whitney, JA; Xu, J; Zhao, Z1
Abella, S; Boxer, M; Hawkins, M; Hu, J; Klein, L; Kolibaba, K; Sharman, J; Wu, M; Yasenchak, C1
Cebrián, D; de Cabo, R; González-García, I; Gutierrez, VM; Iglesias, G; López, M; Lopez-Guadamillas, E; Martinez, S; Mattison, JA; Mitchell, SJ; Muñoz-Martin, M; Ortega-Molina, A; Pastor, J; Serrano, M; Szarowicz, MD; Vaughan, KL1
Greenhill, C1
Chen, K; Gaur, S; Hu, S; Liu, YR; Pan, SL; Tzeng, HE; Wang, Y; Yang, L; Yen, Y1
Abella-Dominicis, E; Barr, PM; Cheson, BD; Di Paolo, J; Dreiling, LK; Friedberg, JW; Greenwald, DR; Hawkins, MJ; He, J; Hu, J; Joshi, A; Lee, H; Liem, AK; Mclntyre, RE; O'Brien, SM; Reddy, A; Saylors, GB; Spurgeon, SE1
Cragg, MS; Hou, S; Marshall, AJ; Pauls, SD; Ray, A; Vaughan, AT1
Choi, JS; Goh, SH; Han, BG; Kim, HS; Kim, JH; Koh, JS; Lee, BI; Lee, J; Lee, SJ; Nam, S; Song, HJ1
Almejún, MB; Bezares, RF; Borge, M; Cabrejo, M; Colado, A; Dos Santos, P; Elías, EE; Fernández Grecco, H; Gamberale, R; Giordano, M; Podaza, E; Risnik, D; Slavutsky, I; Stanganelli, C1
Morimoto-Kamata, R; Yui, S1
Chen, J; Chen, X; Chung, RT; Fuchs, BC; He, L; Holmes, JA; Hong, J; Hu, Q; Jiang, Y; Jin, Q; Li, S; Li, W; Liao, Y; Lidofsky, A; Lin, W; Lin, Z; Liu, Y; Qu, C; Tu, M; Wei, L; Yuan, H; Zheng, D1
Hayashi, T; Kittaka, M; Kondo, T; Reichenberger, EJ; Ueki, Y; Yoshimoto, T1
Alisi, MA; Bettolo, RM; Cazzolla, N; Ceccacci, F; Furlotti, G; Garrone, B; Gasperi, T; La Bella, A; Leonelli, F; Loreto, MA; Magarò, G; Mangano, G; Masini, E; Miceli, M; Migneco, LM; Vitiello, M1
Assouline, S; Burke, JM; Chen, R; Essell, J; Patel-Donnelly, D; Sharman, J; Shi, W; Shustov, A; Yang, J; Ye, W1
Andorsky, DJ; Assouline, S; Forero-Torres, A; Jones, V; Klein, LM; Kolibaba, KS; Patel-Donnelly, D; Sharman, JP; Shi, W; Smith, M; Yasenchak, CA; Ye, W1
Cardona, DM; Cardones, AR; Chao, NJ; Chen, BJ; Di Paolo, JA; Jia, W; Kim, JY; Perez, VL; Poe, JC; Reyes, NJ; Saban, DR; Sarantopoulos, S; Su, H; Sundy, JS1
Assouline, S; Awan, FT; Hill, B; Patel-Donnelly, D; Rao, AV; Sharman, JP; Thirman, MJ; Ye, W1
Alexe, G; Armstrong, SA; Blachly, JS; Byrd, JC; Chu, SH; Cremer, A; Ellegast, JM; Frank, ES; Goodale, A; Häupl, B; Mohr, S; Oellerich, T; Piccioni, F; Pikman, Y; Rao, AV; Robichaud, A; Ross, L; Stegmaier, K; Walker, AR1
Accordi, B; Basso, G; Bresolin, S; Cortese, G; Mariotto, E; Porcù, E; Serafin, V; Veltri, G1
Bhargava, P; Danilov, AV; Dyer, MJS; Fegan, CD; Herbaux, C; Hillmen, P; Huang, X; Humeniuk, R; Jürgensmeier, JM; Karlin, L; Kio, EA; Mitra, SS; Rule, SA; Walter, HS; Yi, PC; Zhou, Z1
Bagashev, A; Brown, PA; Loftus, JP; Niswander, LM; Schauf, A; Tannheimer, S; Tasian, SK; Wang, M; Yahiaoui, A1
Junghanss, C; Kong, W; Murua Escobar, H; Nolte, I; Perez, SV; Ruetgen, B; Sekora, A; Sender, S1
Jorda, R; Krajčovičová, S; Králová, P; Kryštof, V; Soural, M1
Bhatnagar, B; Blachly, JS; Blum, WG; Byrd, JC; Crosswell, HE; Lin, TL; Liu, J; Long, L; Mims, AS; Minden, MD; Munugalavadla, V; Oellerich, T; Orwick, S; Pan, Y; Rao, AV; Serve, H; Walker, AR; Zhang, D1
Bhargava, P; Bouabdallah, K; Cartron, G; Danilov, AV; Davies, AJ; Dyer, MJS; Fegan, C; Hodson, DJ; Huang, X; Humeniuk, R; Jürgensmeier, JM; Li, B; Morschhauser, F; Radford, J; Rajakumaraswamy, N; Rule, SA; Salles, G; Spurgeon, S; Walter, HS; Ysebaert, L1
Becker, A; Chabanovska, O; Junghanss, C; Murua Escobar, H; Ngezahayo, A; Sekora, A; Sender, S; Villa Perez, S1
Best, S; Danilov, AV; Goodyear, S; Hashiguchi, T; Kittai, AS; Lam, V; Okada, C; Park, B; Persky, DO; Spurgeon, SE; Thurlow, B1
Adachi, J; Araki, M; Friboulet, L; Fujita, N; Katayama, K; Katayama, R; Kukimoto-Niino, M; Kutkowska, J; Ma, B; Maruyama, K; Mizuta, H; Nishio, M; Oh-Hara, T; Okada, K; Okuno, Y; Sagae, Y; Sasakura, Y; Shirouzu, M; Simizu, S; Takagi, S; Takemoto, A; Tamai, K; Watanabe, K; Yanagitani, N1
Best, S; Danilov, AV; Kittai, A; Lam, V; Liu, T; Orand, K; Spurgeon, SE1

Reviews

1 review(s) available for pyrazines and indazoles

ArticleYear
Novel molecular targeted therapies for refractory thyroid cancer.
    Head & neck, 2012, Volume: 34, Issue:5

    Topics: Angiogenesis Inhibitors; Anilides; Antineoplastic Agents; Axitinib; Benzamides; Benzenesulfonates; Benzoquinones; Bibenzyls; Boronic Acids; Bortezomib; Depsipeptides; ErbB Receptors; Gefitinib; Histone Deacetylase Inhibitors; HSP90 Heat-Shock Proteins; Humans; Hydroxamic Acids; Imatinib Mesylate; Imidazoles; Indazoles; Indoles; Lactams, Macrocyclic; Lenalidomide; Niacinamide; Oligonucleotides; Phenylurea Compounds; Piperazines; Piperidines; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins c-kit; Pyrazines; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Quinolines; Receptor Protein-Tyrosine Kinases; Receptors, Vascular Endothelial Growth Factor; Sorafenib; Sulfonamides; Sunitinib; Thalidomide; Thyroid Neoplasms; Valproic Acid; Vorinostat

2012

Trials

9 trial(s) available for pyrazines and indazoles

ArticleYear
An open-label phase 2 trial of entospletinib (GS-9973), a selective spleen tyrosine kinase inhibitor, in chronic lymphocytic leukemia.
    Blood, 2015, Apr-09, Volume: 125, Issue:15

    Topics: Aged; Aged, 80 and over; Disease-Free Survival; Female; Humans; Indazoles; Intracellular Signaling Peptides and Proteins; Leukemia, Lymphocytic, Chronic, B-Cell; Male; Middle Aged; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrazines; Syk Kinase

2015
Phase 2 study of idelalisib and entospletinib: pneumonitis limits combination therapy in relapsed refractory CLL and NHL.
    Blood, 2016, 05-19, Volume: 127, Issue:20

    Topics: Adult; Aged; Aged, 80 and over; Antineoplastic Combined Chemotherapy Protocols; Class I Phosphatidylinositol 3-Kinases; Cytokines; Early Termination of Clinical Trials; Female; Humans; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Lymphoma, Non-Hodgkin; Male; Middle Aged; Neoplasm Proteins; Pneumonia; Protein Kinase Inhibitors; Purines; Pyrazines; Quinazolinones; Salvage Therapy; Syk Kinase

2016
An Open-label, Phase II Trial of Entospletinib (GS-9973), a Selective Spleen Tyrosine Kinase Inhibitor, in Diffuse Large B-cell Lymphoma.
    Clinical lymphoma, myeloma & leukemia, 2018, Volume: 18, Issue:8

    Topics: Adult; Aged; Aged, 80 and over; Antineoplastic Agents; Disease Progression; Drug Administration Schedule; Female; Humans; Indazoles; Lymphoma, Large B-Cell, Diffuse; Male; Middle Aged; Progression-Free Survival; Protein Kinase Inhibitors; Pyrazines; Syk Kinase; Time Factors

2018
An open-label phase 2 trial of entospletinib in indolent non-Hodgkin lymphoma and mantle cell lymphoma.
    British journal of haematology, 2019, Volume: 184, Issue:2

    Topics: Adult; Aged; Aged, 80 and over; Female; Humans; Indazoles; Lymphoma, B-Cell, Marginal Zone; Lymphoma, Follicular; Lymphoma, Mantle-Cell; Male; Middle Aged; Neoplasm Proteins; Pyrazines; Syk Kinase; Waldenstrom Macroglobulinemia

2019
Entospletinib monotherapy in patients with relapsed or refractory chronic lymphocytic leukemia previously treated with B-cell receptor inhibitors: results of a phase 2 study.
    Leukemia & lymphoma, 2019, Volume: 60, Issue:8

    Topics: Aged; Aged, 80 and over; Combined Modality Therapy; Drug Resistance, Neoplasm; Female; Humans; Indazoles; Kaplan-Meier Estimate; Leukemia, Lymphocytic, Chronic, B-Cell; Male; Middle Aged; Prognosis; Protein Kinase Inhibitors; Pyrazines; Receptors, Antigen, B-Cell; Recurrence; Retreatment; Treatment Outcome

2019
Phase Ib Study of Tirabrutinib in Combination with Idelalisib or Entospletinib in Previously Treated Chronic Lymphocytic Leukemia.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2020, 06-15, Volume: 26, Issue:12

    Topics: Aged; Aged, 80 and over; Antineoplastic Combined Chemotherapy Protocols; Drug Resistance, Neoplasm; Female; Follow-Up Studies; Humans; Imidazoles; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Male; Maximum Tolerated Dose; Middle Aged; Neoplasm Recurrence, Local; Prognosis; Purines; Pyrazines; Pyrimidines; Quinazolinones; Salvage Therapy; Tissue Distribution

2020
Entospletinib in Combination with Induction Chemotherapy in Previously Untreated Acute Myeloid Leukemia: Response and Predictive Significance of
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2020, 11-15, Volume: 26, Issue:22

    Topics: Adult; Cytarabine; Daunorubicin; Female; Gene Expression Regulation, Neoplastic; Homeodomain Proteins; Humans; Indazoles; Induction Chemotherapy; Leukemia, Myeloid, Acute; Male; Middle Aged; Myeloid Ecotropic Viral Integration Site 1 Protein; Pyrazines; Syk Kinase

2020
Phase 1b study of tirabrutinib in combination with idelalisib or entospletinib in previously treated B-cell lymphoma.
    Leukemia, 2021, Volume: 35, Issue:7

    Topics: Adult; Aged; Antineoplastic Agents; Female; Humans; Imidazoles; Indazoles; Lymphoma, B-Cell; Male; Middle Aged; Protein Kinase Inhibitors; Purines; Pyrazines; Pyrimidines; Quinazolinones

2021
Proapoptotic and immunomodulatory effects of SYK inhibitor entospletinib in combination with obinutuzumab in patients with chronic lymphocytic leukaemia.
    British journal of clinical pharmacology, 2022, Volume: 88, Issue:2

    Topics: Antibodies, Monoclonal, Humanized; Humans; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Neoplasm Recurrence, Local; Pyrazines; Receptors, Antigen, B-Cell; Syk Kinase

2022

Other Studies

26 other study(ies) available for pyrazines and indazoles

ArticleYear
Unprecedented rearrangement of 2-(2-aminoethyl)-1-aryl-3,4-dihydropyrazino[1,2-b]indazole-2-ium 6-oxides to 2,3-dihydro-1H-imidazo[1,2-b]indazoles.
    The Journal of organic chemistry, 2010, Jan-15, Volume: 75, Issue:2

    Topics: Catalysis; Imidazoles; Indazoles; Molecular Structure; Oxides; Pyrazines; Structure-Activity Relationship

2010
2,3,5-Trisubstituted pyridines as selective AKT inhibitors. Part II: Improved drug-like properties and kinase selectivity from azaindazoles.
    Bioorganic & medicinal chemistry letters, 2010, Jan-15, Volume: 20, Issue:2

    Topics: Animals; Cell Line, Tumor; Glycogen Synthase Kinase 3; Glycogen Synthase Kinase 3 beta; Humans; Indazoles; Mice; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Pyrazines; Pyridines; Xenograft Model Antitumor Assays

2010
Discovery and structure-activity relationship of 2,6-disubstituted pyrazines, potent and selective inhibitors of protein kinase CK2.
    Bioorganic & medicinal chemistry letters, 2012, Jul-01, Volume: 22, Issue:13

    Topics: Animals; Binding Sites; Casein Kinase II; Computer Simulation; Disease Models, Animal; Drug Evaluation, Preclinical; Humans; Indazoles; Injections, Intraperitoneal; Nephritis; Protein Kinase Inhibitors; Protein Structure, Tertiary; Pyrazines; Rats; Structure-Activity Relationship

2012
The design and synthesis of indazole and pyrazolopyridine based glucokinase activators for the treatment of type 2 diabetes mellitus.
    Bioorganic & medicinal chemistry letters, 2012, Dec-01, Volume: 22, Issue:23

    Topics: Administration, Oral; Animals; Cell Line, Tumor; Diabetes Mellitus, Type 2; Drug Design; Glucokinase; Glucose Tolerance Test; Half-Life; Humans; Hypoglycemic Agents; Indazoles; Insulin; Kinetics; Protein Binding; Pyrazines; Pyrazoles; Pyridines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship

2012
Strategic use of conformational bias and structure based design to identify potent JAK3 inhibitors with improved selectivity against the JAK family and the kinome.
    Bioorganic & medicinal chemistry letters, 2013, May-01, Volume: 23, Issue:9

    Topics: Binding Sites; Crystallography, X-Ray; Drug Design; Hydrophobic and Hydrophilic Interactions; Indazoles; Janus Kinase 1; Janus Kinase 2; Janus Kinase 3; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Pyrazines; Structure-Activity Relationship

2013
A potential therapeutic strategy for chronic lymphocytic leukemia by combining Idelalisib and GS-9973, a novel spleen tyrosine kinase (Syk) inhibitor.
    Oncotarget, 2014, Feb-28, Volume: 5, Issue:4

    Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Drug Synergism; Humans; Indazoles; Intracellular Signaling Peptides and Proteins; Leukemia, Lymphocytic, Chronic, B-Cell; Phosphorylation; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Purines; Pyrazines; Quinazolinones; Signal Transduction; Syk Kinase

2014
Discovery of GS-9973, a selective and orally efficacious inhibitor of spleen tyrosine kinase.
    Journal of medicinal chemistry, 2014, May-08, Volume: 57, Issue:9

    Topics: Administration, Oral; Animals; Cells, Cultured; Drug Discovery; Humans; Indazoles; Magnetic Resonance Spectroscopy; Mice; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrazines; Rats; Spectrometry, Mass, Electrospray Ionization; Spleen; Structure-Activity Relationship

2014
Pharmacological inhibition of PI3K reduces adiposity and metabolic syndrome in obese mice and rhesus monkeys.
    Cell metabolism, 2015, Apr-07, Volume: 21, Issue:4

    Topics: Adiposity; Animals; Histological Techniques; Imidazoles; Immunoblotting; Indazoles; Liver; Macaca mulatta; Mass Spectrometry; Metabolic Syndrome; Mice, Obese; Phosphoinositide-3 Kinase Inhibitors; Pyrazines; Sulfonamides

2015
Obesity: Inhibiting PI3K reduces body weight in obese mice.
    Nature reviews. Endocrinology, 2015, Volume: 11, Issue:6

    Topics: Adiposity; Animals; Imidazoles; Indazoles; Metabolic Syndrome; Phosphoinositide-3 Kinase Inhibitors; Pyrazines; Sulfonamides

2015
The pan-PI3K inhibitor GDC-0941 activates canonical WNT signaling to confer resistance in TNBC cells: resistance reversal with WNT inhibitor.
    Oncotarget, 2015, May-10, Volume: 6, Issue:13

    Topics: Animals; Apoptosis; beta Catenin; Blotting, Western; Cell Proliferation; Drug Resistance, Neoplasm; Female; Fluorescent Antibody Technique; Humans; Indazoles; Mice; Mice, Nude; Phosphatidylinositol 3-Kinases; Phosphoinositide-3 Kinase Inhibitors; Proto-Oncogene Proteins c-akt; Pyrazines; Pyridines; Real-Time Polymerase Chain Reaction; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Sulfonamides; TOR Serine-Threonine Kinases; Triple Negative Breast Neoplasms; Tumor Cells, Cultured; Wnt Proteins; Xenograft Model Antitumor Assays

2015
FcγRIIB-Independent Mechanisms Controlling Membrane Localization of the Inhibitory Phosphatase SHIP in Human B Cells.
    Journal of immunology (Baltimore, Md. : 1950), 2016, 09-01, Volume: 197, Issue:5

    Topics: B-Lymphocytes; Bridged Bicyclo Compounds, Heterocyclic; Cell Line; Cell Membrane; Cells, Cultured; Green Fluorescent Proteins; Humans; Indazoles; Lymphocyte Activation; Oxazines; Phosphatidylinositol Phosphates; Phosphatidylinositol-3,4,5-Trisphosphate 5-Phosphatases; Photobleaching; Pyrazines; Pyridines; Pyrimidines; Receptors, Antigen, B-Cell; Receptors, IgG; Signal Transduction; Syk Kinase

2016
Crystal structures of spleen tyrosine kinase in complex with novel inhibitors: structural insights for design of anticancer drugs.
    The FEBS journal, 2016, Volume: 283, Issue:19

    Topics: Antineoplastic Agents; Crystallography, X-Ray; Drug Design; Indazoles; Models, Molecular; Oxazines; Protein Kinase Inhibitors; Pyrazines; Pyridines; Syk Kinase

2016
The kinase inhibitors R406 and GS-9973 impair T cell functions and macrophage-mediated anti-tumor activity of rituximab in chronic lymphocytic leukemia patients.
    Cancer immunology, immunotherapy : CII, 2017, Volume: 66, Issue:4

    Topics: Aged; Aged, 80 and over; Cell Proliferation; Cells, Cultured; Female; Humans; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Lymphocyte Activation; Macrophages; Male; Middle Aged; Oxazines; Phagocytosis; Phosphorylation; Pyrazines; Pyridines; Receptors, Antigen, T-Cell; Rituximab; Syk Kinase; T-Lymphocytes; ZAP-70 Protein-Tyrosine Kinase

2017
Insulin-like growth factor-1 signaling is responsible for cathepsin G-induced aggregation of breast cancer MCF-7 cells.
    Cancer science, 2017, Volume: 108, Issue:8

    Topics: Autocrine Communication; Axitinib; Breast Neoplasms; Cathepsin G; Cell Aggregation; Female; Humans; Imidazoles; Indazoles; Indoles; Insulin-Like Growth Factor I; MCF-7 Cells; Phosphorylation; Pyrazines; Pyrroles; Receptor, IGF Type 1; Receptors, Somatomedin; Signal Transduction; Small Molecule Libraries; Sunitinib

2017
Tyrosine kinase SYK is a potential therapeutic target for liver fibrosis.
    Hepatology (Baltimore, Md.), 2018, Volume: 68, Issue:3

    Topics: Animals; Drug Evaluation, Preclinical; Hep G2 Cells; Hepatic Stellate Cells; Hepatocytes; Humans; Indazoles; Liver Cirrhosis, Experimental; Male; Mice, Inbred C57BL; Pyrazines; Rats; Syk Kinase

2018
Second-Generation SYK Inhibitor Entospletinib Ameliorates Fully Established Inflammation and Bone Destruction in the Cherubism Mouse Model.
    Journal of bone and mineral research : the official journal of the American Society for Bone and Mineral Research, 2018, Volume: 33, Issue:8

    Topics: Adaptor Proteins, Signal Transducing; Animals; Bone and Bones; Cherubism; Disease Models, Animal; Indazoles; Inflammation; Mice; Protein Kinase Inhibitors; Pyrazines; Syk Kinase

2018
Targeting Serotonin 2A and Adrenergic α
    ChemMedChem, 2018, 08-10, Volume: 13, Issue:15

    Topics: Animals; Drug Discovery; Indazoles; Intraocular Pressure; Ocular Hypertension; Pyrazines; Rats; Receptor, Serotonin, 5-HT2A; Receptors, Adrenergic, alpha-1; Structure-Activity Relationship

2018
SYK inhibitor entospletinib prevents ocular and skin GVHD in mice.
    JCI insight, 2018, 10-04, Volume: 3, Issue:19

    Topics: Administration, Oral; Animals; B-Lymphocytes; Disease Models, Animal; Drug Evaluation, Preclinical; Eye; Female; Graft vs Host Disease; Hematopoietic Stem Cell Transplantation; Humans; Indazoles; Mice; Protein Kinase Inhibitors; Pyrazines; Skin; Survival Analysis; Syk Kinase; T-Lymphocytes; Treatment Outcome

2018
Resistance Mechanisms to SYK Inhibition in Acute Myeloid Leukemia.
    Cancer discovery, 2020, Volume: 10, Issue:2

    Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Benzamides; Cell Line, Tumor; Clinical Trials, Phase I as Topic; Clinical Trials, Phase II as Topic; Diphenylamine; Drug Resistance, Neoplasm; Drug Synergism; Female; Gene Expression Regulation, Leukemic; Humans; Indazoles; Leukemia, Myeloid, Acute; MAP Kinase Signaling System; Mice; Mitogen-Activated Protein Kinase 1; Mitogen-Activated Protein Kinase Kinases; Mutagenesis, Site-Directed; Mutation; Open Reading Frames; Primary Cell Culture; Protein Kinase Inhibitors; Protein Tyrosine Phosphatase, Non-Receptor Type 11; Pyrazines; Syk Kinase; Xenograft Model Antitumor Assays

2020
SYK Targeting Represents a Potential Therapeutic Option for Relapsed Resistant Pediatric
    International journal of molecular sciences, 2019, Dec-07, Volume: 20, Issue:24

    Topics: Aminopyridines; Cell Proliferation; Child; Core Binding Factor Alpha 2 Subunit; Cyclohexylamines; Drug Resistance, Neoplasm; Humans; Indazoles; Morpholines; Neoplasm Recurrence, Local; Oncogene Proteins, Fusion; Oxazines; Precursor B-Cell Lymphoblastic Leukemia-Lymphoma; Protein Kinase Inhibitors; Pyrazines; Pyridines; Pyrimidines; Syk Kinase; Tumor Cells, Cultured

2019
Combinatorial efficacy of entospletinib and chemotherapy in patient-derived xenograft models of infant acute lymphoblastic leukemia.
    Haematologica, 2021, 04-01, Volume: 106, Issue:4

    Topics: Animals; Heterografts; Humans; Indazoles; Infant; Myeloid-Lymphoid Leukemia Protein; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Pyrazines

2021
Pan- and Isoform-specific Inhibition of the Bromodomain and Extra-terminal Proteins and Evaluation of Synergistic Potential With Entospletinib in Canine Lymphoma.
    Anticancer research, 2020, Volume: 40, Issue:7

    Topics: Animals; Cell Line, Tumor; Dogs; Heterocyclic Compounds, 2-Ring; Heterocyclic Compounds, 4 or More Rings; Indazoles; Lymphoma, Large B-Cell, Diffuse; Nuclear Proteins; Piperazines; Protein Isoforms; Protein Serine-Threonine Kinases; Pyrazines; Pyrazoles; Pyridazines; Syk Kinase

2020
Scaffold hopping of the SYK inhibitor entospletinib leads to broader targeting of the BCR signalosome.
    European journal of medicinal chemistry, 2020, Oct-15, Volume: 204

    Topics: Agammaglobulinaemia Tyrosine Kinase; Dose-Response Relationship, Drug; Humans; Indazoles; Phosphorylation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-bcr; Pyrazines; Signal Transduction; Syk Kinase

2020
Precursor B-ALL Cell Lines Differentially Respond to SYK Inhibition by Entospletinib.
    International journal of molecular sciences, 2021, Jan-08, Volume: 22, Issue:2

    Topics: Apoptosis; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Flow Cytometry; Gene Expression Regulation, Leukemic; Humans; Indazoles; Precursor B-Cell Lymphoblastic Leukemia-Lymphoma; Precursor Cells, B-Lymphoid; Pyrazines; Sequence Analysis, RNA; Syk Kinase

2021
Entospletinib and obinutuzumab in patients with relapsed/refractory chronic lymphocytic leukemia and B-cell malignancies.
    Haematologica, 2021, 07-01, Volume: 106, Issue:7

    Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; B-Lymphocytes; Humans; Indazoles; Leukemia, Lymphocytic, Chronic, B-Cell; Pyrazines

2021
Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer.
    Nature communications, 2021, 02-24, Volume: 12, Issue:1

    Topics: Aminopyridines; Aniline Compounds; Animals; Apoptosis; Benzamides; Carbazoles; Cell Line; Cell Survival; Crizotinib; Drug Resistance, Neoplasm; Enzyme Inhibitors; Humans; Immunoblotting; Indazoles; Lactams; Lactams, Macrocyclic; Lung Neoplasms; Mice; Mice, Inbred BALB C; Molecular Dynamics Simulation; Neoplasm Recurrence, Local; Piperidines; Proto-Oncogene Proteins; Pyrazines; Pyrazoles; Receptor Protein-Tyrosine Kinases

2021