Page last updated: 2024-08-21

isoxazoles and pyrazines

isoxazoles has been researched along with pyrazines in 55 studies

Research

Studies (55)

Timeframe	Studies, this research(%)	All Research%
pre-1990	1 (1.82)	18.7374
1990's	2 (3.64)	18.2507
2000's	5 (9.09)	29.6817
2010's	33 (60.00)	24.3611
2020's	14 (25.45)	2.80

Authors

Authors	Studies
Fotsch, C; St Jean, DJ	1
Dannhardt, G; Dominiak, P; Laufer, S	1
Cheney, DL; McGill, W; Murray, TF	1
Kato, A; Kubo, K; Matsuzaki, Y; Okita, K; Terai, S	1
Chaudhry, V; Umapathi, T	1
Adams, AD; Burton, CA; Chin, J; Guo, Q; Huang, S; Lam, MH; Latham, M; Lopez, JC; Lund, EG; Menke, JG; Milot, DP; Mitnaul, LJ; Peterson, LB; Rex-Rabe, SE; Rosa, RL; Sparrow, CP; Tian, JY; Wright, SD	1
Alcázar, J; Alonso, JM; Alvarez, RM; Andrés, JI; Bakker, MH; Biesmans, I; Cid, JM; De Lucas, AI; Drinkenburg, W; Fernández, J; Font, LM; Iturrino, L; Langlois, X; Lenaerts, I; Martínez, S; Megens, AA; Pastor, J; Pullan, S; Steckler, T	1
Howell, MH; von Arnim, AG; Woo, J	1
Hussar, DA	1
Li, Z; Liu, M; Liu, T; Luo, J; Qiu, WW; Tang, J; Xu, J; Yang, F	1
Gobec, S; Hrast, M; Janežič, D; Konc, J; Turk, S; Vehar, B	1
Brunner, TB; Charlton, PA; Cornelissen, B; Fokas, E; Gillies McKenna, W; Hammond, EM; Muschel, RJ; Olcina, MM; Pollard, JR; Prevo, R; Reaper, PM; Vallis, KA	1
Andrulis, M; Bargou, RC; Beilhack, A; Bogen, B; Bumm, T; Chatterjee, M; Einsele, H; Heimberger, T; Riedel, S; Schraud, H; Stühmer, T	1
Hilgenfeld, R; Jochmans, D; Ma, Q; Nascimento, MS; Neyts, J; Rocha-Pereira, J	1
Boucher, DM; Charlton, P; Charrier, JD; Eustace, B; Furey, B; Golec, J; Gu, Y; Hall, AB; Hare, B; Johnson, MA; Milton, S; Murphy, CE; Newsome, D; Pollard, JR; Reaper, PM; Takemoto, D; Tolman, C; Wang, Y; Wood, M	1
Blacklow, SC; Bradner, JE; Buckley, DL; Fu, H; Huang, Y; Kadam, A; Liu, S; Marineau, JJ; McKeown, MR; Qi, J; Shaw, DL; Xu, X; Zhang, W; Zhang, X; Zhang, Z	1
Bogachkov, Y; Doscas, ME; Kaufman, H; Li, Y; Rao, GS; Ruby, C; Usha, L; Wang, Y; Williams, JW; Williamson, AJ; Xiao, F; Xu, X; Zhou, J	1
Foote, KM; Lau, A; Nissink, JW	1
Altmeyer, R; Gao, Q; Lan, K; Li, G; Wang, Y; Yuan, S; Zou, G	1
Massey, AJ	1
Biskup, E; Gniadecki, R; Naym, DG	1
Gershon, TR; Hwang, D; Kabanov, AV; Lang, PY; Nanjangud, GJ; Parker, JS; Shaw, C; Sokolsky-Papkov, M	1
Boumelha, AJ; Dobrynin, G; Hammond, EM; Hawkins, MA; Ient, J; Leslie, RE; Leszczynska, KB; Maughan, T; Mukherjee, S; Senra, JM	1
Bakkenist, CJ; Beumer, JH; Chu, E; Doyle, A; Iffland, A; Ivy, P; Kiesel, BF; Parise, RA; Scemama, J; Villaruz, L	1
Houghton, PJ; Kang, M; Kurmashev, D; Kurmasheva, RT; Reynolds, CP; Smith, MA; Wu, J	1
Beleggia, F; Büttner, R; Doerr, F; George, J; Hermann, S; Persigehl, T; Rehkämper, T; Reinhardt, HC; Schmitt, A; Thomas, RK; Walter, V; Weber, JP; Wittersheim, M	1
Ding, C; Hao, Y; Liu, M; Qin, Z; Rao, Q; Song, L; Tian, Y; Wang, HW; Wang, J; Wu, Z; Xu, Y	1
Frangou, E; Hawkins, M; Holmes, J; Love, S; McGregor, N	1
Abu-Hashem, AA; El-Shazly, M	1
Chen, KN; Dai, L; Dong, B; Fu, H; Kang, XZ; Liang, Z; Shen, LY; Shi, Q; Xiong, HC; Yan, WP; Yang, YB	1
Fernandez-Capetillo, O; Lecona, E	1
Bindra, RS; Chen, EM; Focarete, ML; Jackson, C; Jiang, Z; Josowitz, AD; Merlettini, A; Noorbakhsh, S; Quijano, AR; Saltzman, WM; Seo, YE; Sundaram, RK	1
Boughey, JC; Goetz, MP; Harmsen, WS; Kahila, MM; Kalari, KR; Lou, Z; Mutter, RW; Sarkaria, JN; Tu, X; Wang, L; Yu, J; Yuan, J; Zhou, Q	1
Badura, J; Becker, H; Fahrer, J; Heylmann, D; Kaina, B	1
Bartfeld, S; Chan, AKW; Chan, AS; Chan, ASY; Chan, D; Cheng, PSW; Clevers, H; Fan, X; Ho, SL; Kwong, DLW; Lam, KO; Law, S; Lee, BCH; Leung, SY; Ma, S; Mak, TW; Man, AHY; Shi, J; Siu, HC; Tsui, WY; Wong, JWH; Yan, HHN; Yue, SSK; Yuen, ST; Zhang, J	1
Chiba, T; Kurian, S; Li, S; Song, Y; Wang, Z; Wu, X; Xiang, R	1
Aben, N; Avelar, AT; Berns, A; Cozijnsen, M; de Vries, H; Nagel, R; Proost, N; van de Ven, M; van der Vliet, J; Wessels, LFA	1
Andrade, AF; Beijersbergen, RL; Bonnefoy, N; Combès, E; Coquel, F; Coquelle, A; Del Rio, M; Desigaud, D; Garambois, V; Gongora, C; Jarlier, M; Martineau, P; Michaud, HA; Moreaux, J; Pasero, P; Tosi, D; Vezzio-Vie, N	1
Li, X; Qi, W; Sun, L; Wang, C; Wang, M; Xu, X; Zhao, D	1
Charrier, JD; Davis, C; Durrant, S; Golec, J; Griffiths, M; Kay, D; Knegtel, R; Littlewood, P; MacCormick, S; O'Donnell, M; Pinder, J; Pollard, J; Reaper, P; Storck, P; Twin, H; Virani, A; Young, S	1
Bindra, RS; Breslin, H; Burgenske, DM; Ganesa, S; Gilad, O; Jackson, CB; Jia, L; Kalathil, AN; Noorbakhsh, SI; Sarkaria, JN; Sundaram, RK	1
Andrs, M; Gorecki, L; Korabecny, J; Rezacova, M	1
Algéo, MP; Chaire, V; Italiano, A; Laroche-Clary, A; Le Loarer, F; Malykh, A; Verbeke, S	1
Distel, L; Dobler, C; Fietkau, R; Hecht, M; Jost, T	1
Falk, M; Hendriks, BS; Jansen, M; Terranova, N	1
Arumugaswami, V; Bakowski, MA; Bartenschlager, R; Beck, S; Betz, UAK; Beutler, N; Chatterjee, AK; Damoiseaux, RD; Gabriel, G; Garcia, G; Gomperts, B; Han, B; Kim, H; Kirkpatrick, MG; Kohn, DB; Parcells, MS; Purbey, PK; Purkayastha, A; Ramaiah, A; Riva, L; Rogers, TF; Scumpia, P; Sen, C; Sharma, A; Svendsen, CN; Ulmert, D; Wolff, KC; Yuen, C	1
Aladjem, MI; Beck, E; Ceribelli, M; Chen, L; Dahmen, H; Desai, P; Elenbaas, B; Figg, WD; Itkin, Z; Khan, J; Kim, S; Kindrick, JD; Klumpp-Thomas, C; Lee, MJ; Lee, S; McKnight, C; Michael, S; Nichols, S; Peer, CJ; Pommier, Y; Puc, J; Rajapakse, VN; Redon, CE; Schultz, CW; Sciuto, L; Shimellis, H; Steinberg, SM; Sun, Y; Takahashi, N; Thomas, A; Thomas, CJ; Travers, J; Trepel, JB; Varonin, J; Wei, JS; Wilson, KM; Yuno, A; Zenke, FT; Zhang, X; Zhang, Y; Zimmermann, A	1
Elloumi, F; Jo, U; Kim, SH; Murai, Y; Pommier, Y; Rajapakse, VN; Saha, LK; Schultz, CW; Senatorov, IS; Takahashi, N; Thomas, A; Zenke, FT; Zimmermann, A	1
Bürkel, F; Distel, LV; Faulhaber, EM; Fietkau, R; Hecht, M; Jost, T; Scheper, J; Symank, J	1
Abel, L; Baschnagel, AM; Clark, PA; Elnaggar, JH; Kaushik, S; Kimple, RJ; Kromke, AC; Leal, TA; Longhurst, CA; Nickel, KP; Skiba, JH; VanBeek, HJ; Zhao, SG	1
Cui, Y; Dreicer, R; Emamekhoo, H; Frankel, PH; Hoimes, C; Kim, WY; Lara, PN; Lyou, Y; Michaelson, D; Milowsky, M; Mortazavi, A; Newman, E; Pal, SK; Parikh, M; Parikh, R; Srinivas, S; Teply, B; Vaishampayan, U; Weng, P; Zhang, T	1
Fu, F; Geng, Z; Hu, L; Huang, Q; Li, X; Liu, S; Liu, X; Song, Q; Wang, H; Yin, Q; Zhu, Y	1
Cheng, SC; Chowdhury, D; Curtis, J; D'Andrea, AD; da Costa, AABA; Färkkilä, A; Gulhan, D; Hendrickson, AEW; Kochupurakkal, B; Kohn, EC; Kolin, DL; Konstantinopoulos, PA; Lee, EK; Liu, JF; Matulonis, UA; Polak, M; Shapiro, GI; Stover, EH; Tayob, N	1
Bindra, RS; Burgenske, DM; Dragojevic, S; Elmquist, WF; Gupta, SK; Kim, M; Mohammad, AS; Sarkaria, JN; Talele, S; Zhang, W	1
Classe, JM; Ferron, G; Floquet, A; Freyer, G; Hardy-Bessard, AC; Kurtz, JE; Lécuru, F; Motte-Rouge, T; Pautier, P	1

Reviews

6 review(s) available for isoxazoles and pyrazines

Article	Year
Mitigating heterocycle metabolism in drug discovery. Journal of medicinal chemistry, 2012, Jul-12, Volume: 55, Issue:13 Topics: Animals; Biotransformation; Databases, Factual; Drug Discovery; Drug Interactions; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds, 4 or More Rings; Humans; Mice; Pharmaceutical Preparations; Rats	2012
Toxic neuropathy. Current opinion in neurology, 2005, Volume: 18, Issue:5 Topics: Animals; Boronic Acids; Bortezomib; Clinical Trials as Topic; Epothilones; Genetic Therapy; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Isoxazoles; Leflunomide; Neuritis; Neuroprotective Agents; Neurotoxicity Syndromes; Organoplatinum Compounds; Oxaliplatin; Peripheral Nervous System Diseases; Pyrazines; Pyridoxine; Thalidomide	2005
Drugging ATR: progress in the development of specific inhibitors for the treatment of cancer. Future medicinal chemistry, 2015, Volume: 7, Issue:7 Topics: Antineoplastic Agents; Ataxia Telangiectasia Mutated Proteins; DNA Damage; Humans; Isoxazoles; Molecular Conformation; Neoplasms; Pyrazines	2015
Targeting ATR in cancer. Nature reviews. Cancer, 2018, Volume: 18, Issue:9 Topics: Ataxia Telangiectasia Mutated Proteins; DNA Damage; Drug Development; Genomic Instability; Humans; Indoles; Isoxazoles; Molecular Targeted Therapy; Morpholines; Neoplasms; Nitroso Compounds; Oxazines; Protein Kinase Inhibitors; Pyrazines; Pyrimidines; Quinolines; Sulfonamides; Sulfoxides	2018
Discovery of ATR kinase inhibitor berzosertib (VX-970, M6620): Clinical candidate for cancer therapy. Pharmacology & therapeutics, 2020, Volume: 210 Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Drug Discovery; Drug Synergism; Humans; Isoxazoles; Molecular Targeted Therapy; Neoplasms; Protein Kinase Inhibitors; Pyrazines; Signal Transduction; Sulfones; Treatment Outcome	2020
Prise en charge médicale de la récidive du cancer épithélial de l'ovaire: Medical management of recurrent epithelial ovarian cancer. Bulletin du cancer, 2021, Volume: 108, Issue:9S1 Topics: Antibodies, Monoclonal, Humanized; Antineoplastic Agents, Immunological; Antineoplastic Combined Chemotherapy Protocols; Azepines; Bevacizumab; Carcinoma, Ovarian Epithelial; Female; Genes, BRCA1; Genes, BRCA2; Humans; Immunoconjugates; Immunotherapy; Isoxazoles; Maintenance Chemotherapy; Maytansine; Neoplasm Recurrence, Local; Ovarian Neoplasms; Platinum Compounds; Poly(ADP-ribose) Polymerase Inhibitors; Pteridines; Pyrazines; Pyrimidines	2021

Trials

3 trial(s) available for isoxazoles and pyrazines

Article	Year
Population pharmacokinetics of ATR inhibitor berzosertib in phase I studies for different cancer types. Cancer chemotherapy and pharmacology, 2021, Volume: 87, Issue:2 Topics: Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Dose-Response Relationship, Drug; Female; Humans; Infusions, Intravenous; Inhibitory Concentration 50; Isoxazoles; Male; Middle Aged; Models, Biological; Neoplasms; Protein Kinase Inhibitors; Pyrazines	2021
Effect of Cisplatin and Gemcitabine With or Without Berzosertib in Patients With Advanced Urothelial Carcinoma: A Phase 2 Randomized Clinical Trial. JAMA oncology, 2021, Oct-01, Volume: 7, Issue:10 Topics: Aged; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Transitional Cell; Cisplatin; Deoxycytidine; Gemcitabine; Humans; Isoxazoles; Male; Pyrazines; Treatment Outcome; Urinary Bladder Neoplasms	2021
A Replication stress biomarker is associated with response to gemcitabine versus combined gemcitabine and ATR inhibitor therapy in ovarian cancer. Nature communications, 2021, 09-22, Volume: 12, Issue:1 Topics: Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Biomarkers, Tumor; Deoxycytidine; DNA Replication; Female; Gemcitabine; Humans; Isoxazoles; Mutation; Oncogenes; Ovarian Neoplasms; Progression-Free Survival; Protein Kinase Inhibitors; Pyrazines; Recombinational DNA Repair; Retinoblastoma Binding Proteins	2021

Other Studies

46 other study(ies) available for isoxazoles and pyrazines

Article	Year
[Hypertensive action of 5-(beta-aminoethyl)aminoisoxazoles: synthesis and screening of isoxazolopyrazines and isoxazolodiazepines]. Archiv der Pharmazie, 1991, Volume: 324, Issue:3 Topics: Animals; Azepines; Blood Pressure; Decerebrate State; Heart Rate; Isoxazoles; Male; Pyrazines; Rats; Rats, Inbred Strains; Structure-Activity Relationship	1991
A comparison of the analgesic activities of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol (THIP) and 6-chloro-2[1-piperazinyl]pyrazine (MK 212). European journal of pharmacology, 1983, Jun-03, Volume: 90, Issue:2-3 Topics: Analgesics; Animals; Bicuculline; Dose-Response Relationship, Drug; Drug Synergism; Drug Tolerance; Isoxazoles; Male; Mice; Morphine; Oxazoles; Pyrazines; Time Factors	1983
Antitumor effect of vesnarinone on human hepatocellular carcinoma cell lines. International journal of oncology, 1999, Volume: 14, Issue:1 Topics: Antineoplastic Agents; Apoptosis; Carcinoma, Hepatocellular; Cell Division; Dose-Response Relationship, Drug; Humans; In Situ Nick-End Labeling; Isoxazoles; Liver Neoplasms; Pyrazines; Quinolines; Tumor Cells, Cultured	1999
Different roles of liver X receptor alpha and beta in lipid metabolism: effects of an alpha-selective and a dual agonist in mice deficient in each subtype. Biochemical pharmacology, 2006, Feb-14, Volume: 71, Issue:4 Topics: 8-Bromo Cyclic Adenosine Monophosphate; Administration, Oral; Animals; ATP Binding Cassette Transporter 1; ATP-Binding Cassette Transporters; Cholesterol; Cholesterol, HDL; Cyclic AMP; DNA-Binding Proteins; Dose-Response Relationship, Drug; Gene Expression Regulation; Isoxazoles; Lipid Metabolism; Liver; Liver X Receptors; Macrophages, Peritoneal; Mice; Mice, Inbred C57BL; Mice, Knockout; Molecular Structure; Orphan Nuclear Receptors; Phenylurea Compounds; Protein Isoforms; Pyrazines; Receptors, Cytoplasmic and Nuclear; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Sterol Regulatory Element Binding Protein 1; Triglycerides	2006
Tricyclic isoxazolines: identification of R226161 as a potential new antidepressant that combines potent serotonin reuptake inhibition and alpha2-adrenoceptor antagonism. Bioorganic & medicinal chemistry, 2007, Jun-01, Volume: 15, Issue:11 Topics: Adrenergic alpha-2 Receptor Antagonists; Animals; Antidepressive Agents, Tricyclic; Humans; Isoxazoles; Male; Oxazoles; Pyrazines; Rats; Rats, Wistar; Selective Serotonin Reuptake Inhibitors	2007
Structure-function studies on the active site of the coelenterazine-dependent luciferase from Renilla. Protein science : a publication of the Protein Society, 2008, Volume: 17, Issue:4 Topics: Aequorin; Amino Acid Sequence; Binding Sites; Catalysis; Computer Simulation; Diethyl Pyrocarbonate; Imidazoles; Isoxazoles; Luciferases, Renilla; Luminescent Measurements; Models, Molecular; Mutagenesis, Site-Directed; Phenylmethylsulfonyl Fluoride; Pyrazines; Structure-Activity Relationship	2008
New drug update: 2007. The Consultant pharmacist : the journal of the American Society of Consultant Pharmacists, 2008, Volume: 23, Issue:4 Topics: Aged; Amides; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antihypertensive Agents; Antiparkinson Agents; Antipsychotic Agents; Drug Approval; Fumarates; Humans; Hypoglycemic Agents; Isoxazoles; Macular Degeneration; Paliperidone Palmitate; Pyrazines; Pyrimidines; Ranibizumab; Sitagliptin Phosphate; Tetrahydronaphthalenes; Thiophenes; Triazoles; United States	2008
Synthesis and biological evaluation of heterocyclic ring-fused betulinic acid derivatives as novel inhibitors of osteoclast differentiation and bone resorption. Journal of medicinal chemistry, 2012, Apr-12, Volume: 55, Issue:7 Topics: Acid Phosphatase; Animals; Betulinic Acid; Bone Density Conservation Agents; Bone Resorption; Cathepsin K; Cell Differentiation; Cell Line; Cell Proliferation; Crystallography, X-Ray; Female; Isoenzymes; Isoxazoles; Mice; Mice, Inbred C57BL; Osteoclasts; Ovariectomy; Pentacyclic Triterpenes; Pyrazines; Pyrazoles; Pyrimidines; RANK Ligand; Rats; Structure-Activity Relationship; Tartrate-Resistant Acid Phosphatase; Thiazoles; Triterpenes	2012
Function of the D-alanine:D-alanine ligase lid loop: a molecular modeling and bioactivity study. Journal of medicinal chemistry, 2012, Aug-09, Volume: 55, Issue:15 Topics: Bacterial Proteins; Benzothiazoles; Enzyme Assays; Escherichia coli Proteins; Isoxazoles; Molecular Dynamics Simulation; Peptide Synthases; Protein Binding; Protein Conformation; Pyrazines; Pyrimidines; Stereoisomerism; Structure-Activity Relationship; Thermus	2012
Targeting ATR in vivo using the novel inhibitor VE-822 results in selective sensitization of pancreatic tumors to radiation. Cell death & disease, 2012, Dec-06, Volume: 3 Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Cell Cycle Proteins; Cell Line, Tumor; Cell Survival; Checkpoint Kinase 1; DNA Damage; Female; Humans; Isoxazoles; Mice; Mice, Inbred BALB C; Pancreatic Neoplasms; Phosphorylation; Protein Kinase Inhibitors; Protein Kinases; Protein Serine-Threonine Kinases; Pyrazines; Radiation Tolerance; Radiation-Sensitizing Agents	2012
The heat shock transcription factor 1 as a potential new therapeutic target in multiple myeloma. British journal of haematology, 2013, Volume: 160, Issue:4 Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Blotting, Western; Boronic Acids; Bortezomib; Cells, Cultured; Diterpenes; DNA-Binding Proteins; Down-Regulation; Epoxy Compounds; Female; Gene Knockdown Techniques; Heat Shock Transcription Factors; Heat-Shock Proteins; Humans; Immunohistochemistry; Isoxazoles; Mice; Mice, Inbred BALB C; Multiple Myeloma; Neoplasm Transplantation; Phenanthrenes; Plasma Cells; Proteasome Endopeptidase Complex; Pyrazines; Resorcinols; RNA, Small Interfering; Transcription Factors; Transplantation, Heterologous	2013
The enterovirus protease inhibitor rupintrivir exerts cross-genotypic anti-norovirus activity and clears cells from the norovirus replicon. Antimicrobial agents and chemotherapy, 2014, Volume: 58, Issue:8 Topics: Amides; Antiviral Agents; Cell Line; Cysteine Endopeptidases; Cytidine; Drug Combinations; Drug Synergism; Hepatocytes; Humans; Isoxazoles; Molecular Docking Simulation; Norwalk virus; Papain; Phenylalanine; Pyrazines; Pyrrolidinones; Replicon; RNA-Dependent RNA Polymerase; Valine; Viral Proteins; Virus Replication	2014
Potentiation of tumor responses to DNA damaging therapy by the selective ATR inhibitor VX-970. Oncotarget, 2014, Jul-30, Volume: 5, Issue:14 Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; Cisplatin; DNA; DNA Damage; Drug Synergism; Female; Humans; Isoxazoles; Mice; Mice, SCID; Phosphorylation; Protein Kinase Inhibitors; Pyrazines; Random Allocation; Signal Transduction; Xenograft Model Antitumor Assays	2014
Biased multicomponent reactions to develop novel bromodomain inhibitors. Journal of medicinal chemistry, 2014, Nov-13, Volume: 57, Issue:21 Topics: Alkanesulfonic Acids; Azepines; Cell Cycle Proteins; Cell Line, Tumor; Crystallography, X-Ray; Fluorocarbons; Gene Expression Regulation; Humans; Imidazoles; Inhibitory Concentration 50; Isoxazoles; Ligands; Models, Molecular; Nuclear Proteins; Pyrazines; Pyridines; Small Molecule Libraries; Structure-Activity Relationship; Transcription Factors	2014
Inhibition of p70 S6 kinase (S6K1) activity by A77 1726 and its effect on cell proliferation and cell cycle progress. Neoplasia (New York, N.Y.), 2014, Volume: 16, Issue:10 Topics: Aniline Compounds; Butadienes; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Chromones; Crotonates; Feedback, Physiological; Gene Knockdown Techniques; Humans; Hydroxybutyrates; Imidazoles; Isoxazoles; Leflunomide; MAP Kinase Signaling System; Morpholines; Nitriles; Phosphatidylinositol 3-Kinases; Protein Kinase Inhibitors; Pyrazines; Receptor, IGF Type 1; Ribosomal Protein S6 Kinases, 70-kDa; Toluidines	2014
In Vitro Assessment of Combinations of Enterovirus Inhibitors against Enterovirus 71. Antimicrobial agents and chemotherapy, 2016, Volume: 60, Issue:9 Topics: Amides; Amino Acid Sequence; Animals; Antiviral Agents; Binding Sites; Cell Line, Tumor; Chlorocebus aethiops; Drug Combinations; Drug Resistance, Viral; Drug Synergism; Enterovirus A, Human; Humans; Indoles; Isoxazoles; Itraconazole; Molecular Docking Simulation; Mutation; Myoblasts; Phenols; Phenylalanine; Protein Binding; Protein Interaction Domains and Motifs; Protein Structure, Secondary; Pyrazines; Pyrrolidinones; Sequence Alignment; Sequence Homology, Amino Acid; Suramin; Valine; Vero Cells; Viral Nonstructural Proteins; Virus Replication	2016
Inhibition of ATR-dependent feedback activation of Chk1 sensitises cancer cells to Chk1 inhibitor monotherapy. Cancer letters, 2016, 12-01, Volume: 383, Issue:1 Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Bone Neoplasms; Cell Proliferation; Checkpoint Kinase 1; Colorectal Neoplasms; DNA Damage; DNA-Activated Protein Kinase; Dose-Response Relationship, Drug; Histones; HT29 Cells; Humans; Indoles; Isoxazoles; Molecular Targeted Therapy; Nuclear Proteins; Osteosarcoma; Protein Kinase Inhibitors; Pyrazines; Pyridones; Signal Transduction; Time Factors	2016
Small-molecule inhibitors of Ataxia Telangiectasia and Rad3 related kinase (ATR) sensitize lymphoma cells to UVA radiation. Journal of dermatological science, 2016, Volume: 84, Issue:3 Topics: Ataxia Telangiectasia Mutated Proteins; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Cell Survival; Checkpoint Kinase 1; Flow Cytometry; Histones; Humans; Isoxazoles; Lymphoma, T-Cell, Cutaneous; Phosphorylation; Photochemotherapy; Photosensitizing Agents; Pyrazines; Quinolines; Quinuclidines; RNA, Small Interfering; Sulfones; Tumor Cells, Cultured; Ultraviolet Rays	2016
ATR maintains chromosomal integrity during postnatal cerebellar neurogenesis and is required for medulloblastoma formation. Development (Cambridge, England), 2016, 11-01, Volume: 143, Issue:21 Topics: Animals; Animals, Newborn; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Transformation, Neoplastic; Cerebellar Neoplasms; Cerebellum; Chromosomal Instability; Developmental Disabilities; Female; Gene Deletion; Gene Expression Regulation, Developmental; Gene Expression Regulation, Neoplastic; Isoxazoles; Male; Medulloblastoma; Mice; Mice, Inbred C57BL; Mice, Knockout; Nervous System Malformations; Neurogenesis; Neurons; Pyrazines	2016
Preclinical testing of an Atr inhibitor demonstrates improved response to standard therapies for esophageal cancer. Radiotherapy and oncology : journal of the European Society for Therapeutic Radiology and Oncology, 2016, Volume: 121, Issue:2 Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; Chemoradiotherapy; Esophageal Neoplasms; Humans; Isoxazoles; Mice; Pyrazines	2016
LC-MS/MS assay for the quantitation of the ATR kinase inhibitor VX-970 in human plasma. Journal of pharmaceutical and biomedical analysis, 2017, Nov-30, Volume: 146 Topics: Ataxia Telangiectasia Mutated Proteins; Biological Assay; Chromatography, Liquid; Formates; Humans; Isoxazoles; Plasma; Pyrazines; Reproducibility of Results; Spectrometry, Mass, Electrospray Ionization; Tandem Mass Spectrometry	2017
Initial testing (stage 1) of M6620 (formerly VX-970), a novel ATR inhibitor, alone and combined with cisplatin and melphalan, by the Pediatric Preclinical Testing Program. Pediatric blood & cancer, 2018, Volume: 65, Issue:2 Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; Cisplatin; Female; Humans; Isoxazoles; Melphalan; Mice; Mice, SCID; Neoplasms, Experimental; Protein Kinase Inhibitors; Pyrazines; Xenograft Model Antitumor Assays	2018
Targeting a non-oncogene addiction to the ATR/CHK1 axis for the treatment of small cell lung cancer. Scientific reports, 2017, Nov-14, Volume: 7, Issue:1 Topics: Adenocarcinoma of Lung; Animals; Antineoplastic Agents; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Benzodiazepinones; cdc25 Phosphatases; Cell Cycle; Cell Line, Tumor; Checkpoint Kinase 1; DNA Damage; Drug Resistance, Neoplasm; Gene Expression Regulation, Neoplastic; Humans; Isoxazoles; Lung Neoplasms; Male; Mice; Mice, Nude; Molecular Targeted Therapy; Protein Kinase Inhibitors; Proto-Oncogene Proteins p21(ras); Pyrazines; Pyrazoles; RNA, Messenger; Signal Transduction; Small Cell Lung Carcinoma; Xenograft Model Antitumor Assays	2017
Cryo-EM structure of human ATR-ATRIP complex. Cell research, 2018, Volume: 28, Issue:2 Topics: Adaptor Proteins, Signal Transducing; Ataxia Telangiectasia Mutated Proteins; Carrier Proteins; Chromatography, Affinity; Chromatography, Gel; Cryoelectron Microscopy; DNA Damage; DNA-Binding Proteins; Humans; Isoxazoles; Mutation; Nuclear Proteins; Phosphorylation; Protein Binding; Protein Conformation, alpha-Helical; Protein Folding; Protein Kinases; Protein Multimerization; Pyrazines; Signal Transduction; TOR Serine-Threonine Kinases	2018
Challenges in implementing model-based phase I designs in a grant-funded clinical trials unit. Trials, 2017, Dec-28, Volume: 18, Issue:1 Topics: Clinical Trials, Phase I as Topic; Combined Modality Therapy; Esophageal Neoplasms; Humans; Isoxazoles; Maximum Tolerated Dose; Pyrazines; Research Design	2017
Synthesis of New Isoxazole-, Pyridazine-, Pyrimidopyrazines and Their Anti-Inflammatory and Analgesic Activity. Medicinal chemistry (Shariqah (United Arab Emirates)), 2018, Volume: 14, Issue:4 Topics: Analgesics; Animals; Anti-Inflammatory Agents, Non-Steroidal; Drug Evaluation, Preclinical; Female; Isoxazoles; Male; Mice; Molecular Structure; Pyrazines; Pyridazines; Pyrimidines; Rats, Sprague-Dawley	2018
The identification of the ATR inhibitor VE-822 as a therapeutic strategy for enhancing cisplatin chemosensitivity in esophageal squamous cell carcinoma. Cancer letters, 2018, 09-28, Volume: 432 Topics: Animals; Antineoplastic Agents; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Carcinoma, Squamous Cell; Cell Cycle; Cell Proliferation; Cisplatin; CRISPR-Cas Systems; Drug Resistance, Neoplasm; Esophageal Neoplasms; Female; Gene Expression Regulation, Neoplastic; Humans; Isoxazoles; Mice; Mice, Inbred BALB C; Mice, Nude; Prognosis; Pyrazines; Signal Transduction; Survival Rate; Tumor Cells, Cultured; Xenograft Model Antitumor Assays	2018
Biodegradable PEG-poly(ω-pentadecalactone-co-p-dioxanone) nanoparticles for enhanced and sustained drug delivery to treat brain tumors. Biomaterials, 2018, Volume: 178 Topics: Animals; Biocompatible Materials; Brain Neoplasms; Convection; Drug Delivery Systems; Drug Liberation; Hydrodynamics; Isoxazoles; Male; Nanoparticles; Polyesters; Polyethylene Glycols; Pyrazines; Radiation-Sensitizing Agents; Rats, Inbred F344; Xenograft Model Antitumor Assays	2018
ATR Inhibition Is a Promising Radiosensitizing Strategy for Triple-Negative Breast Cancer. Molecular cancer therapeutics, 2018, Volume: 17, Issue:11 Topics: Animals; Ataxia Telangiectasia Mutated Proteins; cdc25 Phosphatases; Cell Cycle Checkpoints; Cell Line, Tumor; Checkpoint Kinase 1; DNA Breaks, Double-Stranded; Drug Resistance, Neoplasm; Female; Homologous Recombination; Humans; Isoxazoles; Mice, Inbred NOD; Mice, SCID; Phosphorylation; Proteolysis; Pyrazines; Radiation-Sensitizing Agents; Triple Negative Breast Neoplasms; Xenograft Model Antitumor Assays	2018
Sensitivity of CD3/CD28-stimulated versus non-stimulated lymphocytes to ionizing radiation and genotoxic anticancer drugs: key role of ATM in the differential radiation response. Cell death & disease, 2018, 10-15, Volume: 9, Issue:11 Topics: Amino Acid Chloromethyl Ketones; Antibodies; Ataxia Telangiectasia Mutated Proteins; Caspases; CD28 Antigens; CD3 Complex; Cell Proliferation; Chromones; DNA-Activated Protein Kinase; Drug Resistance; Gamma Rays; Gene Expression Regulation; Humans; Isoxazoles; Lymphocyte Activation; Morpholines; MRE11 Homologue Protein; Primary Cell Culture; Pyrazines; Pyrones; Radiation Tolerance; Signal Transduction; T-Lymphocytes, Cytotoxic; T-Lymphocytes, Regulatory; Thiophenes; Thioxanthenes	2018
A Comprehensive Human Gastric Cancer Organoid Biobank Captures Tumor Subtype Heterogeneity and Enables Therapeutic Screening. Cell stem cell, 2018, 12-06, Volume: 23, Issue:6 Topics: Aminopyridines; Antineoplastic Agents; Benzimidazoles; Benzofurans; Biological Specimen Banks; Cell Proliferation; Drug Screening Assays, Antitumor; Female; Humans; Isoxazoles; Male; Naphthoquinones; Organoids; Precision Medicine; Pyrazines; Stomach Neoplasms	2018
DNA polymerase θ (POLQ) is important for repair of DNA double-strand breaks caused by fork collapse. The Journal of biological chemistry, 2019, 03-15, Volume: 294, Issue:11 Topics: Camptothecin; Cells, Cultured; DNA Breaks, Double-Stranded; DNA Polymerase theta; DNA Repair; DNA Replication; DNA-Directed DNA Polymerase; Dose-Response Relationship, Drug; Humans; Isoxazoles; Protein Kinase Inhibitors; Pyrazines; Structure-Activity Relationship; Topoisomerase Inhibitors	2019
Inhibition of the Replication Stress Response Is a Synthetic Vulnerability in SCLC That Acts Synergistically in Combination with Cisplatin. Molecular cancer therapeutics, 2019, Volume: 18, Issue:4 Topics: A549 Cells; Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Survival; Checkpoint Kinase 1; Cisplatin; CRISPR-Associated Protein 9; DNA Damage; Drug Synergism; Etoposide; Humans; Isoxazoles; Lung Neoplasms; Mice; Mice, Inbred BALB C; Mice, Nude; Protein Kinase Inhibitors; Pyrazines; Small Cell Lung Carcinoma; Tumor Burden; Xenograft Model Antitumor Assays	2019
Inhibition of Ataxia-Telangiectasia Mutated and RAD3-Related ( Cancer research, 2019, 06-01, Volume: 79, Issue:11 Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; Checkpoint Kinase 2; Colorectal Neoplasms; DNA Breaks, Double-Stranded; Drug Resistance, Neoplasm; Female; Humans; Isoxazoles; Mice, Inbred C57BL; Oxaliplatin; Pyrazines; T-Lymphocytes; Xenograft Model Antitumor Assays	2019
Inhibition of Wee1 sensitizes AML cells to ATR inhibitor VE-822-induced DNA damage and apoptosis. Biochemical pharmacology, 2019, Volume: 164 Topics: Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Cycle Proteins; DNA Damage; Dose-Response Relationship, Drug; Humans; Isoxazoles; Leukemia, Myeloid, Acute; Protein-Tyrosine Kinases; Pyrazines; U937 Cells	2019
Rational Design of 5-(4-(Isopropylsulfonyl)phenyl)-3-(3-(4-((methylamino)methyl)phenyl)isoxazol-5-yl)pyrazin-2-amine (VX-970, M6620): Optimization of Intra- and Intermolecular Polar Interactions of a New Ataxia Telangiectasia Mutated and Rad3-Related (ATR Journal of medicinal chemistry, 2019, 06-13, Volume: 62, Issue:11 Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Cell Line; Drug Design; Isoxazoles; Male; Models, Molecular; Protein Conformation; Protein Kinase Inhibitors; Pyrazines; Rats; Rats, Sprague-Dawley	2019
Temozolomide Sensitizes MGMT-Deficient Tumor Cells to ATR Inhibitors. Cancer research, 2019, 09-01, Volume: 79, Issue:17 Topics: Animals; Antineoplastic Agents, Alkylating; Antineoplastic Combined Chemotherapy Protocols; Ataxia Telangiectasia Mutated Proteins; Cell Cycle Checkpoints; Cell Line, Tumor; Checkpoint Kinase 1; DNA Breaks, Double-Stranded; DNA Damage; DNA Modification Methylases; DNA Repair Enzymes; Drug Synergism; Female; Humans; Isoxazoles; Mice, Nude; Pyrazines; Temozolomide; Tumor Suppressor Proteins; Xenograft Model Antitumor Assays	2019
ATR Inhibition Broadly Sensitizes Soft-Tissue Sarcoma Cells to Chemotherapy Independent of Alternative Lengthening Telomere (ALT) Status. Scientific reports, 2020, 05-04, Volume: 10, Issue:1 Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Cell Line, Tumor; DNA Damage; Female; Humans; Isoxazoles; Mice; Mice, Knockout; Neoplasm Proteins; Pyrazines; S Phase Cell Cycle Checkpoints; Sarcoma; Telomere Homeostasis; Xenograft Model Antitumor Assays	2020
Senescence Induction by Combined Ionizing Radiation and DNA Damage Response Inhibitors in Head and Neck Squamous Cell Carcinoma Cells. Cells, 2020, 09-01, Volume: 9, Issue:9 Topics: Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Cycle; Cell Line, Tumor; Cellular Senescence; DNA Damage; Fibroblasts; Head and Neck Neoplasms; Humans; Isoxazoles; Male; Protein Kinase Inhibitors; Pyrazines; Pyridines; Quinolines; Radiation, Ionizing; Signal Transduction; Squamous Cell Carcinoma of Head and Neck; TOR Serine-Threonine Kinases; Triazoles	2020
Antiviral drug screen identifies DNA-damage response inhibitor as potent blocker of SARS-CoV-2 replication. Cell reports, 2021, 04-06, Volume: 35, Issue:1 Topics: A549 Cells; Animals; Antiviral Agents; Chlorocebus aethiops; COVID-19; COVID-19 Drug Treatment; DNA Damage; Drug Evaluation, Preclinical; HEK293 Cells; HeLa Cells; Humans; Isoxazoles; MAP Kinase Signaling System; Middle East Respiratory Syndrome Coronavirus; Pyrazines; SARS-CoV-2; Vero Cells; Virus Replication	2021
Therapeutic targeting of ATR yields durable regressions in small cell lung cancers with high replication stress. Cancer cell, 2021, 04-12, Volume: 39, Issue:4 Topics: Aged; Antineoplastic Agents; Ataxia Telangiectasia Mutated Proteins; DNA Replication; DNA Topoisomerases, Type I; Genomic Instability; Humans; Isoxazoles; Lung Neoplasms; Middle Aged; Neoplasm Recurrence, Local; Protein Kinase Inhibitors; Pyrazines; Signal Transduction; Small Cell Lung Carcinoma	2021
Novel and Highly Potent ATR Inhibitor M4344 Kills Cancer Cells With Replication Stress, and Enhances the Chemotherapeutic Activity of Widely Used DNA Damaging Agents. Molecular cancer therapeutics, 2021, Volume: 20, Issue:8 Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Ataxia Telangiectasia Mutated Proteins; Cell Proliferation; Deoxycytidine; DNA Replication; Female; Gemcitabine; Gene Expression Regulation, Neoplastic; Humans; Irinotecan; Isoxazoles; Lung Neoplasms; Mice; Mice, Nude; Morpholines; Pyrazines; Pyrazoles; Small Cell Lung Carcinoma; Topotecan; Tumor Cells, Cultured; Xenograft Model Antitumor Assays	2021
Kinase Inhibitors of DNA-PK, ATM and ATR in Combination with Ionizing Radiation Can Increase Tumor Cell Death in HNSCC Cells While Sparing Normal Tissue Cells. Genes, 2021, 06-17, Volume: 12, Issue:6 Topics: Ataxia Telangiectasia Mutated Proteins; Carcinoma, Squamous Cell; Cell Death; Cell Line, Tumor; Cells, Cultured; DNA Repair; DNA-Activated Protein Kinase; Head and Neck Neoplasms; Humans; Isoxazoles; Protein Kinase Inhibitors; Pyrazines; Pyridines; Quinolines; Triazoles; X-Rays	2021
ATR Inhibitor M6620 (VX-970) Enhances the Effect of Radiation in Non-Small Cell Lung Cancer Brain Metastasis Patient-Derived Xenografts. Molecular cancer therapeutics, 2021, Volume: 20, Issue:11 Topics: Animals; Carcinoma, Non-Small-Cell Lung; Female; Heterografts; Humans; Isoxazoles; Lung Neoplasms; Mice; Mice, Nude; Neoplasm Metastasis; Pyrazines; Treatment Outcome	2021
VE-822, a novel DNA Holliday junction stabilizer, inhibits homologous recombination repair and triggers DNA damage response in osteogenic sarcomas. Biochemical pharmacology, 2021, Volume: 193 Topics: Antineoplastic Agents; Cell Line, Tumor; DNA; DNA Damage; DNA Repair; Doxorubicin; Humans; Isoxazoles; Osteosarcoma; Pyrazines; Recombination, Genetic	2021
Brain Distribution of Berzosertib: An Ataxia Telangiectasia and Rad3-Related Protein Inhibitor for the Treatment of Glioblastoma. The Journal of pharmacology and experimental therapeutics, 2021, Volume: 379, Issue:3 Topics: Animals; Ataxia Telangiectasia Mutated Proteins; Brain; Cell Line, Tumor; Female; Glioblastoma; HEK293 Cells; Humans; Infusion Pumps; Isoxazoles; Male; Mice; Mice, Knockout; Mice, Nude; Pyrazines; Xenograft Model Antitumor Assays	2021