Page last updated: 2024-09-03

gefitinib and zd 6474

gefitinib has been researched along with zd 6474 in 54 studies

Compound Research Comparison

Studies
(gefitinib)
Trials
(gefitinib)
Recent Studies (post-2010)
(gefitinib)
Studies
(zd 6474)
Trials
(zd 6474)
Recent Studies (post-2010) (zd 6474)
5,2315662,91962388413

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)zd 6474 (IC50)
Tyrosine-protein kinase ABL1Homo sapiens (human)0.1185
Epidermal growth factor receptorHomo sapiens (human)0.5373
Macrophage colony-stimulating factor 1 receptorHomo sapiens (human)1.6
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)0.7738
Platelet-derived growth factor receptor betaHomo sapiens (human)0.7885
Mast/stem cell growth factor receptor KitHomo sapiens (human)0.343
Fibroblast growth factor receptor 1Homo sapiens (human)2.7925
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)0.0769
Vascular endothelial growth factor receptor 1 Homo sapiens (human)0.5812
Kinesin-1 heavy chainHomo sapiens (human)0.4
Vascular endothelial growth factor receptor 3Homo sapiens (human)0.1464
Vascular endothelial growth factor receptor 2Homo sapiens (human)0.5425
Angiopoietin-1 receptorHomo sapiens (human)1.5335
Macrophage-stimulating protein receptorHomo sapiens (human)3.37
Coiled-coil domain-containing protein 6Homo sapiens (human)0.02
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)0.2

Research

Studies (54)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's26 (48.15)29.6817
2010's24 (44.44)24.3611
2020's4 (7.41)2.80

Authors

AuthorsStudies
Atteridge, CE; Azimioara, MD; Benedetti, MG; Biggs, WH; Carter, TA; Ciceri, P; Edeen, PT; Fabian, MA; Floyd, M; Ford, JM; Galvin, M; Gerlach, JL; Grotzfeld, RM; Herrgard, S; Insko, DE; Insko, MA; Lai, AG; Lélias, JM; Lockhart, DJ; Mehta, SA; Milanov, ZV; Patel, HK; Treiber, DK; Velasco, AM; Wodicka, LM; Zarrinkar, PP1
Ballard, P; Bradbury, RH; Harris, CS; Hennequin, LF; Hickinson, M; Kendrew, J; Kettle, JG; Klinowska, T; Ogilvie, DJ; Pearson, SE; Williams, EJ; Wilson, I1
Cheung, K; Dushin, RG; Floyd, MB; Fraser, HL; Ingalls, CL; Loganzo, F; Nittoli, T; Ravi, MR; Tan, X; Wissner, A1
Atteridge, CE; Campbell, BT; Chan, KW; Ciceri, P; Davis, MI; Edeen, PT; Faraoni, R; Floyd, M; Gallant, P; Herrgard, S; Hunt, JP; Karaman, MW; Lockhart, DJ; Milanov, ZV; Morrison, MJ; Pallares, G; Patel, HK; Pritchard, S; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Barnes, JC; Bradley, P; Day, NC; Fourches, D; Reed, JZ; Tropsha, A1
Hajduk, PJ; Johnson, EF; Kifle, L; Merta, PJ; Metz, JT; Soni, NB1
Depreux, P; Farce, A; Garofalo, A; Goossens, L; Lemoine, A; Ravez, S; Six, P1
Russu, WA; Shallal, HM1
Dubey, PK; Pal, M; Piedrafita, FJ; Rajitha, C; Sunku, V; Veeramaneni, VR1
Ciceri, P; Davis, MI; Herrgard, S; Hocker, M; Hunt, JP; Pallares, G; Treiber, DK; Wodicka, LM; Zarrinkar, PP1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Aiche, S; Bassermann, F; Becker, W; Canevari, G; Casale, E; Depaolini, SR; Ehrlich, HC; Felder, ER; Feuchtinger, A; Garz, AK; Gohlke, BO; Götze, K; Greif, PA; Hahne, H; Heinzlmeir, S; Helm, D; Huenges, J; Jeremias, I; Kayser, G; Klaeger, S; Koch, H; Koenig, PA; Kramer, K; Kuster, B; Médard, G; Meng, C; Petzoldt, S; Polzer, H; Preissner, R; Qiao, H; Reinecke, M; Reiter, K; Rueckert, L; Ruland, J; Ruprecht, B; Schlegl, J; Schmidt, T; Schneider, S; Schoof, M; Spiekermann, K; Tõnisson, N; Vick, B; Vooder, T; Walch, A; Wilhelm, M; Wu, Z; Zecha, J; Zolg, DP1
Das, D; Hong, J1
Asquith, CRM; Drewry, DH; East, MP; Havener, TM; Johnson, GL; Laitinen, T; Morris, DC; Naegeli, KM; Wells, CI; Zuercher, WJ1
Chang, J; Chu, J; He, Y; Li, Y; Qi, C; Wang, Y; Xu, P1
Chen, XB; Wang, S; Wang, SQ; Yu, B; Yuan, XH; Zhao, W1
Caballero, E; García-Cárceles, J; Gil, C; Martínez, A1
Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF1
Shiotsu, Y1
Koh, Y; Koizumi, F; Nishio, K; Saijo, N; Taguchi, F; Tamura, T1
Arao, T; Fukumoto, H; Nishio, K; Saijo, N; Takeda, M; Tamura, T1
Brave, S; Kendrew, J; Stratford, IJ; Telfer, BA; Wedge, SR; Whittaker, L; Williams, KJ1
Cascone, T; Ciardiello, F; De Vita, F; Eckhardt, SG; Laus, G; Morelli, MP; Orditura, M; Pepe, S; Tortora, G; Troiani, T1
Heymach, JV1
Lee, D1
Bianco, R; Cascone, T; Ciardiello, F; De Pacido, S; Eckhardt, SG; Fontanini, G; Morelli, MP; Normanno, N; Romano, M; Tortora, G; Troiani, T; Tuccillo, C; Veneziani, BM1
Goto, H; Matsumori, Y; Nakataki, E; Ryan, AJ; Sone, S; Wedge, SR; Yano, S1
Azzariti, A; Paradiso, A; Porcelli, L; Simone, GM; Xu, JM1
Burchert, A; Dietrich, C; Gläser, S; Hoffmann, S; Lingelbach, S; Müller, H; Rothmund, M; Wunderlich, A; Zielke, A1
Frederick, B; Gustafson, DL; Merz, AL; Raben, D1
Antonaci, S; Azzariti, A; Giannelli, G; Paradiso, A; Porcelli, L; Sgarra, C1
Giordano, S; Petrelli, A1
Goto, H; Hanibuchi, M; Ikuta, K; Kakiuchi, S; Nakataki, E; Nishioka, Y; Ogino, H; Ryan, A; Sone, S; Yamada, T; Yano, S1
Berrino, L; Cascone, T; Ciardiello, F; Heymach, JV; Kim, WY; Lee, HY; Morelli, MP; Morgillo, F; Pepe, S; Rodolico, G; Tortora, G1
Sherman, SI2
Bemis, LT; Flaig, TW; Li, Y; McCoach, C; Raben, D; Su, LJ; Varella-Garcia, M1
Bodkin, D; Capó, A; Eberhardt, WE; Germonpré, P; Govindan, R; Kennedy, SJ; Natale, RB; Ranson, M; Rizvi, NA; Sleckman, BG; Stockman, PK1
Akslen, LA; Briggs, A; Byers, LA; Cascone, T; Engelman, J; Folkman, J; Halmos, B; Heymach, JV; Jänne, P; Johnson, BE; Kobayashi, S; Lifshits, E; Naumov, GN; Nilsson, MB; Straume, O; Tang, XM; Tenen, D; Wu, HK; Xu, L; Yeap, B1
Azzariti, A; Berardi, F; Colabufo, NA; D'Incalci, M; Paradiso, A; Perrone, R; Porcelli, L; Quatrale, AE; Simone, GM; Xu, JM; Zucchetti, M1
Dziadziusko, R; Fennell, D; Gridelli, C; Lacombe, D; Pallis, AG; Serfass, L; van Meerbeeck, JP; Welch, J1
Bischoff, H; Kindermann, M; Reinmuth, N; Steins, MB; Thomas, M1
Friedrich, MJ1
Arango, BA; Cohen, EE; Perez, CA; Raez, LE; Santos, ES1
Baryawno, N; Ekström, TJ; Johnsen, JI; Larsson, C; Marino, AM; Sofiadis, A; Vukojević, V1
Berrino, L; Cascone, T; Ciardiello, F; D'Aiuto, E; De Palma, R; Heymach, JV; Martinelli, E; Morgillo, F; Saintigny, P; Troiani, T; Tuccillo, C1
Antalffy, G; Hegedüs, C; Kéri, G; Német, K; Orfi, L; Ozvegy-Laczka, C; Sarkadi, B; Settleman, J; Szakács, G; Truta-Feles, K; Váradi, A; Várady, G1
Aburatani, H; Endo, S; Fukayama, M; Ishikawa, S; Kanai, Y; Kataoka, H; Matsubara, D; Murakami, Y; Niki, T; Oguni, S; Ohara, S; Sakatani, T; Tamura, T; Yoshimoto, T1
Beijnen, JH; Harmsen, S; Maas-Bakker, RF; Meijerman, I; Schellens, JH1
Cass, CE; Damaraju, VL; Kuzma, M; Mowles, D; Ryan, AJ; Sawyer, MB; Scriver, T1
Chang, H; Kim, HS; Kim, JW; Lee, JS; Moon, SU; Sung, JH1
Kang, Y; Ma, W; Yang, L; Yang, T; Zhu, M1
Li, XF; Liu, GF; Miao, YY; Yu, SN; Zhang, SH1
Al-Zubaidi, Y; Bourget, K; Murray, M; Rahman, MK; Tam, S; Zhou, F1

Reviews

14 review(s) available for gefitinib and zd 6474

ArticleYear
Recent advancements of 4-aminoquinazoline derivatives as kinase inhibitors and their applications in medicinal chemistry.
    European journal of medicinal chemistry, 2019, May-15, Volume: 170

    Topics: Animals; Antineoplastic Agents; Chemistry Techniques, Synthetic; Humans; Neoplasms; Protein Kinase Inhibitors; Quinazolines

2019
FDA-approved pyrimidine-fused bicyclic heterocycles for cancer therapy: Synthesis and clinical application.
    European journal of medicinal chemistry, 2021, Mar-15, Volume: 214

    Topics: Antineoplastic Agents; Bridged Bicyclo Compounds, Heterocyclic; Humans; Molecular Structure; Neoplasms; Pyrimidines; United States; United States Food and Drug Administration

2021
Kinase Inhibitors as Underexplored Antiviral Agents.
    Journal of medicinal chemistry, 2022, 01-27, Volume: 65, Issue:2

    Topics: Animals; Antiviral Agents; Drug Repositioning; Humans; Protein Kinase Inhibitors; Virus Diseases; Viruses

2022
Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
    European journal of medicinal chemistry, 2022, Jul-05, Volume: 237

    Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; Breast Neoplasms; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Female; Humans; Neoplasm Proteins; Neoplastic Stem Cells

2022
[Current screening for molecular target therapy of cancer].
    Gan to kagaku ryoho. Cancer & chemotherapy, 2003, Volume: 30, Issue:12

    Topics: Angiogenesis Inhibitors; Animals; Antineoplastic Agents; Benzamides; Boronic Acids; Bortezomib; Drug Delivery Systems; Drug Screening Assays, Antitumor; Gefitinib; Heat-Shock Proteins; Humans; Imatinib Mesylate; Indoles; Lactones; Mice; Neoplasms; Phthalazines; Piperazines; Piperidines; Pyrazines; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Sunitinib

2003
ZD6474--clinical experience to date.
    British journal of cancer, 2005, Volume: 92 Suppl 1

    Topics: Administration, Oral; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Non-Small-Cell Lung; Clinical Trials, Phase I as Topic; Clinical Trials, Phase II as Topic; Drug Administration Schedule; ErbB Receptors; Gefitinib; Humans; Lung Neoplasms; Neovascularization, Pathologic; Piperidines; Quinazolines; Vascular Endothelial Growth Factor A

2005
Phase II data with ZD6474, a small-molecule kinase inhibitor of epidermal growth factor receptor and vascular endothelial growth factor receptor, in previously treated advanced non-small-cell lung cancer.
    Clinical lung cancer, 2005, Volume: 7, Issue:2

    Topics: Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Non-Small-Cell Lung; Clinical Trials, Phase II as Topic; Docetaxel; ErbB Receptors; Gefitinib; Humans; Lung Neoplasms; Piperidines; Protein Kinase Inhibitors; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Taxoids

2005
From single- to multi-target drugs in cancer therapy: when aspecificity becomes an advantage.
    Current medicinal chemistry, 2008, Volume: 15, Issue:5

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Benzamides; Benzenesulfonates; Bevacizumab; Cetuximab; Clinical Trials as Topic; Enzyme Inhibitors; Erlotinib Hydrochloride; Gefitinib; Humans; Imatinib Mesylate; Indoles; Lapatinib; Neoplasms; Neovascularization, Pathologic; Niacinamide; Phenylurea Compounds; Piperazines; Piperidines; Protein-Tyrosine Kinases; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Receptor Protein-Tyrosine Kinases; Sorafenib; Sunitinib; Trastuzumab

2008
Early clinical studies of novel therapies for thyroid cancers.
    Endocrinology and metabolism clinics of North America, 2008, Volume: 37, Issue:2

    Topics: Angiogenesis Inhibitors; Antineoplastic Agents; Axitinib; Benzamides; Benzenesulfonates; Carcinoma; Clinical Trials as Topic; Drug Delivery Systems; Gefitinib; Humans; Imatinib Mesylate; Imidazoles; Indazoles; Indoles; Niacinamide; Oligonucleotides; Phenylurea Compounds; Piperazines; Piperidines; Protein Kinase Inhibitors; Pyridines; Pyrimidines; Quinazolines; Sorafenib; Thyroid Neoplasms

2008
Targeted therapies in the treatment of advanced/metastatic NSCLC.
    European journal of cancer (Oxford, England : 1990), 2009, Volume: 45, Issue:14

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Benzenesulfonates; Bevacizumab; Carcinoma, Non-Small-Cell Lung; Cetuximab; Erlotinib Hydrochloride; Gefitinib; Humans; Indoles; Lung Neoplasms; Niacinamide; Phenylurea Compounds; Piperidines; Pyridines; Pyrroles; Quinazolines; Sorafenib; Sunitinib; Treatment Outcome

2009
Tyrosine kinase inhibitors and the thyroid.
    Best practice & research. Clinical endocrinology & metabolism, 2009, Volume: 23, Issue:6

    Topics: Axitinib; Benzenesulfonates; Clinical Trials as Topic; Gefitinib; Humans; Imidazoles; Indazoles; Indoles; Niacinamide; Oligonucleotides; Pharmaceutical Preparations; Phenylurea Compounds; Piperidines; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Proto-Oncogene Proteins B-raf; Pyridines; Pyrimidines; Pyrroles; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Sorafenib; Sulfonamides; Sunitinib; Thyroid Gland; Thyroid Neoplasms

2009
Targeting the epidermal growth factor receptor in non-small cell lung cancer.
    Onkologie, 2010, Volume: 33, Issue:12

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Non-Small-Cell Lung; Cetuximab; Clinical Trials as Topic; Drug Delivery Systems; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lung Neoplasms; Piperidines; Protein Kinase Inhibitors; Quinazolines

2010
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
Efficacy and adverse events of five targeted agents in the treatment of advanced or metastatic non-small-cell lung cancer: A network meta-analysis of nine eligible randomized controlled trials involving 5,059 patients.
    Journal of cellular physiology, 2019, Volume: 234, Issue:4

    Topics: Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Crown Ethers; Disease Progression; Erlotinib Hydrochloride; Gefitinib; Humans; Lung Neoplasms; Molecular Targeted Therapy; Network Meta-Analysis; Piperidines; Progression-Free Survival; Protein Kinase Inhibitors; Quinazolines; Quinazolinones; Randomized Controlled Trials as Topic

2019

Trials

1 trial(s) available for gefitinib and zd 6474

ArticleYear
Vandetanib versus gefitinib in patients with advanced non-small-cell lung cancer: results from a two-part, double-blind, randomized phase ii study.
    Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 2009, May-20, Volume: 27, Issue:15

    Topics: Adult; Aged; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cross-Over Studies; Disease-Free Survival; Double-Blind Method; Female; Gefitinib; Humans; Kaplan-Meier Estimate; Lung Neoplasms; Male; Middle Aged; Piperidines; Quinazolines

2009

Other Studies

39 other study(ies) available for gefitinib and zd 6474

ArticleYear
A small molecule-kinase interaction map for clinical kinase inhibitors.
    Nature biotechnology, 2005, Volume: 23, Issue:3

    Topics: Benzamides; Drug Design; Escherichia coli; Escherichia coli Proteins; Imatinib Mesylate; Microchemistry; Pharmaceutical Preparations; Piperazines; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Pyrimidines

2005
Inhibitors of epidermal growth factor receptor tyrosine kinase: optimisation of potency and in vivo pharmacokinetics.
    Bioorganic & medicinal chemistry letters, 2006, Sep-15, Volume: 16, Issue:18

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Chemical Phenomena; Chemistry, Physical; ErbB Receptors; Fluorine; Gefitinib; Humans; Inhibitory Concentration 50; Mice; Molecular Structure; Neoplasms; Protein Kinase Inhibitors; Quinazolines; Rats; Structure-Activity Relationship; Thiazoles; Xenograft Model Antitumor Assays

2006
Dual irreversible kinase inhibitors: quinazoline-based inhibitors incorporating two independent reactive centers with each targeting different cysteine residues in the kinase domains of EGFR and VEGFR-2.
    Bioorganic & medicinal chemistry, 2007, Jun-01, Volume: 15, Issue:11

    Topics: Adenosine Triphosphate; Binding Sites; Biological Assay; Cells, Cultured; ErbB Receptors; Humans; Inhibitory Concentration 50; Models, Molecular; Molecular Structure; Protein Conformation; Protein Kinase Inhibitors; Quinazolines; Vascular Endothelial Growth Factor Receptor-2

2007
A quantitative analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2008, Volume: 26, Issue:1

    Topics: Binding Sites; Enzyme Activation; Humans; Phosphotransferases; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Proteome; Quantitative Structure-Activity Relationship

2008
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
    Chemical research in toxicology, 2010, Volume: 23, Issue:1

    Topics: Animals; Chemical and Drug Induced Liver Injury; Cluster Analysis; Databases, Factual; Humans; MEDLINE; Mice; Models, Chemical; Molecular Conformation; Quantitative Structure-Activity Relationship

2010
Navigating the kinome.
    Nature chemical biology, 2011, Volume: 7, Issue:4

    Topics: Drug Design; Pharmacogenetics; Protein Kinases; Proteome; Systems Biology

2011
Impact of aryloxy-linked quinazolines: a novel series of selective VEGFR-2 receptor tyrosine kinase inhibitors.
    Bioorganic & medicinal chemistry letters, 2011, Apr-01, Volume: 21, Issue:7

    Topics: Cell Line, Tumor; Cell Proliferation; Humans; Models, Molecular; Quinazolines; Receptor Protein-Tyrosine Kinases; Structure-Activity Relationship; Vascular Endothelial Growth Factor Receptor-2

2011
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:6

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Molecular Structure; Piperazines; Protein Kinase Inhibitors; Protein Kinases; Pyrimidines; Stereoisomerism; Structure-Activity Relationship

2011
Synthesis and pharmacological evaluations of novel 2H-benzo[b][1,4]oxazin-3(4H)-one derivatives as a new class of anti-cancer agents.
    European journal of medicinal chemistry, 2011, Volume: 46, Issue:10

    Topics: Antineoplastic Agents; Benzene Derivatives; Cell Line, Tumor; Drug Screening Assays, Antitumor; Humans; Neoplasms; Oxazines; Structure-Activity Relationship

2011
Comprehensive analysis of kinase inhibitor selectivity.
    Nature biotechnology, 2011, Oct-30, Volume: 29, Issue:11

    Topics: Catalysis; Drug Design; Enzyme Stability; High-Throughput Screening Assays; Humans; Protein Binding; Protein Kinase Inhibitors; Protein Kinases; Proteomics; Signal Transduction; Substrate Specificity

2011
Identification of potent Yes1 kinase inhibitors using a library screening approach.
    Bioorganic & medicinal chemistry letters, 2013, Aug-01, Volume: 23, Issue:15

    Topics: Binding Sites; Cell Line; Cell Survival; Drug Design; Humans; Hydrogen Bonding; Molecular Docking Simulation; Protein Kinase Inhibitors; Protein Structure, Tertiary; Proto-Oncogene Proteins c-yes; Small Molecule Libraries; Structure-Activity Relationship

2013
The target landscape of clinical kinase drugs.
    Science (New York, N.Y.), 2017, 12-01, Volume: 358, Issue:6367

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cytokines; Drug Discovery; fms-Like Tyrosine Kinase 3; Humans; Leukemia, Myeloid, Acute; Lung Neoplasms; Mice; Molecular Targeted Therapy; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proteomics; Xenograft Model Antitumor Assays

2017
Design of a Cyclin G Associated Kinase (GAK)/Epidermal Growth Factor Receptor (EGFR) Inhibitor Set to Interrogate the Relationship of EGFR and GAK in Chordoma.
    Journal of medicinal chemistry, 2019, 05-09, Volume: 62, Issue:9

    Topics: Aminoquinolines; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Chordoma; Drug Design; ErbB Receptors; HEK293 Cells; Humans; Intracellular Signaling Peptides and Proteins; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Quinazolines

2019
Novel promising 4-anilinoquinazoline-based derivatives as multi-target RTKs inhibitors: Design, molecular docking, synthesis, and antitumor activities in vitro and vivo.
    Bioorganic & medicinal chemistry, 2019, 10-15, Volume: 27, Issue:20

    Topics: Aniline Compounds; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Molecular Docking Simulation; Molecular Structure; Protein Kinase Inhibitors; Quinazolines; Reactive Oxygen Species; Receptor Protein-Tyrosine Kinases; Structure-Activity Relationship

2019
Anticancer effects of ZD6474, a VEGF receptor tyrosine kinase inhibitor, in gefitinib ("Iressa")-sensitive and resistant xenograft models.
    Cancer science, 2004, Volume: 95, Issue:12

    Topics: Adenocarcinoma; Animals; Antineoplastic Agents; Apoptosis; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Drug Resistance, Neoplasm; Enzyme Inhibitors; Female; Gefitinib; Lung Neoplasms; Mice; Mice, Nude; Neovascularization, Pathologic; Phosphorylation; Piperidines; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Tumor Cells, Cultured; Tyrosine; Xenograft Model Antitumor Assays

2004
Small in-frame deletion in the epidermal growth factor receptor as a target for ZD6474.
    Cancer research, 2004, Dec-15, Volume: 64, Issue:24

    Topics: Base Sequence; Cell Line, Tumor; Gefitinib; Gene Deletion; Genes, erbB-1; Humans; Molecular Sequence Data; Neoplasms; Piperidines; Quinazolines; Transfection; Vascular Endothelial Growth Factor Receptor-2

2004
ZD6474, a potent inhibitor of vascular endothelial growth factor signaling, combined with radiotherapy: schedule-dependent enhancement of antitumor activity.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2004, Dec-15, Volume: 10, Issue:24

    Topics: Animals; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Combined Modality Therapy; Endothelial Cells; Female; Gefitinib; Humans; Lung Neoplasms; Mice; Mice, Nude; Oxygen; Piperidines; Quinazolines; Radiotherapy; Signal Transduction; Vascular Endothelial Growth Factor A; Vascular Endothelial Growth Factor Receptor-2; Xenograft Model Antitumor Assays

2004
Sequence-dependent antiproliferative effects of cytotoxic drugs and epidermal growth factor receptor inhibitors.
    Annals of oncology : official journal of the European Society for Medical Oncology, 2005, Volume: 16 Suppl 4

    Topics: Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Carboplatin; Carcinoma, Squamous Cell; Cell Cycle; Cell Line, Tumor; Cetuximab; Cisplatin; Docetaxel; Dose-Response Relationship, Drug; ErbB Receptors; Esophageal Neoplasms; Gefitinib; Humans; Organoplatinum Compounds; Oxaliplatin; Paclitaxel; Piperidines; Quinazolines; Taxoids

2005
Anti-tumor activity of the combination of cetuximab, an anti-EGFR blocking monoclonal antibody and ZD6474, an inhibitor of VEGFR and EGFR tyrosine kinases.
    Journal of cellular physiology, 2006, Volume: 208, Issue:2

    Topics: Animals; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Cetuximab; Drug Evaluation, Preclinical; Drug Therapy, Combination; ErbB Receptors; Female; Gefitinib; Humans; Mice; Mice, Nude; Piperidines; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Xenograft Model Antitumor Assays

2006
ZD6474, an inhibitor of vascular endothelial growth factor receptor tyrosine kinase, inhibits growth of experimental lung metastasis and production of malignant pleural effusions in a non-small cell lung cancer model.
    Oncology research, 2006, Volume: 16, Issue:1

    Topics: Angiogenesis Inhibitors; Animals; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Proliferation; Endothelium, Vascular; Enzyme-Linked Immunosorbent Assay; ErbB Receptors; Flow Cytometry; Gefitinib; Humans; Immunohistochemistry; Lung Neoplasms; Male; Mice; Mice, Inbred BALB C; Neoplasm Transplantation; Neoplasms, Experimental; Neovascularization, Pathologic; Piperidines; Pleural Effusion, Malignant; Quinazolines; Reverse Transcriptase Polymerase Chain Reaction; Vascular Endothelial Growth Factor Receptor-2

2006
Prolonged exposure of colon cancer cells to the epidermal growth factor receptor inhibitor gefitinib (Iressa(TM)) and to the antiangiogenic agent ZD6474: Cytotoxic and biomolecular effects.
    World journal of gastroenterology, 2006, Aug-28, Volume: 12, Issue:32

    Topics: Antineoplastic Combined Chemotherapy Protocols; Cell Line, Tumor; Chromatography, High Pressure Liquid; Colonic Neoplasms; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; ErbB Receptors; Gefitinib; Humans; Inhibitory Concentration 50; Piperidines; Quinazolines; Signal Transduction; Time Factors

2006
Targeting the EGF/VEGF-R system by tyrosine-kinase inhibitors--a novel antiproliferative/antiangiogenic strategy in thyroid cancer.
    Langenbeck's archives of surgery, 2006, Volume: 391, Issue:6

    Topics: Carcinoma; Cell Culture Techniques; Cell Line, Tumor; Cell Proliferation; ErbB Receptors; Gefitinib; Humans; Piperidines; Protein Kinase Inhibitors; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Thyroid Neoplasms; Vascular Endothelial Growth Factor A

2006
Dose scheduling of the dual VEGFR and EGFR tyrosine kinase inhibitor vandetanib (ZD6474, Zactima) in combination with radiotherapy in EGFR-positive and EGFR-null human head and neck tumor xenografts.
    Cancer chemotherapy and pharmacology, 2008, Volume: 61, Issue:2

    Topics: Animals; Blotting, Western; Cell Line, Tumor; Cell Proliferation; Combined Modality Therapy; ErbB Receptors; Gefitinib; Head and Neck Neoplasms; Humans; Mice; Mice, Inbred BALB C; Mice, Nude; Neoplasm Transplantation; Piperidines; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Signal Transduction; Vascular Endothelial Growth Factor Receptor-2; Xenograft Model Antitumor Assays

2008
EGFR and VEGFR as potential target for biological therapies in HCC cells.
    Cancer letters, 2008, Apr-18, Volume: 262, Issue:2

    Topics: Carcinoma, Hepatocellular; Cell Line, Tumor; Drug Delivery Systems; ErbB Receptors; Gefitinib; Humans; Liver Neoplasms; Piperidines; Quinazolines; Receptors, Vascular Endothelial Growth Factor

2008
Novel dual targeting strategy with vandetanib induces tumor cell apoptosis and inhibits angiogenesis in malignant pleural mesothelioma cells expressing RET oncogenic rearrangement.
    Cancer letters, 2008, Jun-28, Volume: 265, Issue:1

    Topics: Angiogenesis Inhibitors; Animals; Apoptosis; Base Sequence; Cell Line, Tumor; Cell Proliferation; ErbB Receptors; Gefitinib; Gene Rearrangement; Humans; Male; Mesothelioma; Mice; Mice, SCID; Molecular Sequence Data; Neoplasm Transplantation; Neovascularization, Pathologic; Piperidines; Pleural Neoplasms; Proto-Oncogene Proteins c-ret; Quinazolines; Transplantation, Heterologous; Vascular Endothelial Growth Factor Receptor-2

2008
Synergistic anti-proliferative and pro-apoptotic activity of combined therapy with bortezomib, a proteasome inhibitor, with anti-epidermal growth factor receptor (EGFR) drugs in human cancer cells.
    Journal of cellular physiology, 2008, Volume: 216, Issue:3

    Topics: Animals; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Agents; Apoptosis; Boronic Acids; Bortezomib; Cell Line, Tumor; Cetuximab; Dose-Response Relationship, Drug; Drug Combinations; Drug Synergism; Enzyme Activation; ErbB Receptors; Gefitinib; Humans; Mitogen-Activated Protein Kinases; Piperidines; Proteasome Endopeptidase Complex; Proteasome Inhibitors; Proto-Oncogene Proteins c-akt; Pyrazines; Quinazolines; Signal Transduction

2008
Dual epidermal growth factor receptor and vascular endothelial growth factor receptor inhibition with vandetanib sensitizes bladder cancer cells to cisplatin in a dose- and sequence-dependent manner.
    BJU international, 2009, Volume: 103, Issue:12

    Topics: Antineoplastic Combined Chemotherapy Protocols; Blotting, Western; Cell Line, Tumor; Cisplatin; Dose-Response Relationship, Drug; Drug Synergism; ErbB Receptors; Gefitinib; Humans; In Situ Hybridization, Fluorescence; Piperidines; Quinazolines; Urinary Bladder Neoplasms; Vascular Endothelial Growth Factors

2009
Combined vascular endothelial growth factor receptor and epidermal growth factor receptor (EGFR) blockade inhibits tumor growth in xenograft models of EGFR inhibitor resistance.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2009, May-15, Volume: 15, Issue:10

    Topics: Animals; Antibodies, Monoclonal; Antibodies, Monoclonal, Humanized; Antineoplastic Combined Chemotherapy Protocols; Bevacizumab; Blotting, Western; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lung Neoplasms; Mice; Mice, Nude; Mutation; NIH 3T3 Cells; Piperidines; Quinazolines; Receptors, Vascular Endothelial Growth Factor; Reverse Transcriptase Polymerase Chain Reaction; Time Factors; Transfection; Tumor Burden; Vascular Endothelial Growth Factor A; Xenograft Model Antitumor Assays

2009
Tyrosine kinase inhibitors and multidrug resistance proteins: interactions and biological consequences.
    Cancer chemotherapy and pharmacology, 2010, Volume: 65, Issue:2

    Topics: Animals; Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Biological Transport; Camptothecin; Cell Line; Cell Line, Tumor; Dogs; Doxorubicin; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Gefitinib; Humans; Irinotecan; Mitoxantrone; Neoplasm Proteins; Piperidines; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Time Factors

2010
NSCLC drug targets acquire new visibility.
    Journal of the National Cancer Institute, 2011, Mar-02, Volume: 103, Issue:5

    Topics: Antineoplastic Agents; Benzenesulfonates; Benzimidazoles; Bexarotene; Biomarkers, Tumor; Carcinoma, Non-Small-Cell Lung; Crizotinib; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lung Neoplasms; Molecular Targeted Therapy; Mutation; Niacinamide; Oncogene Proteins, Fusion; Phenylurea Compounds; Piperidines; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrazoles; Pyridines; Quinazolines; Randomized Controlled Trials as Topic; Sorafenib; Tetrahydronaphthalenes; Treatment Outcome

2011
Enhanced effects by 4-phenylbutyrate in combination with RTK inhibitors on proliferation in brain tumor cell models.
    Biochemical and biophysical research communications, 2011, Jul-22, Volume: 411, Issue:1

    Topics: Antineoplastic Combined Chemotherapy Protocols; Brain Neoplasms; Cell Line, Tumor; Cell Proliferation; Cell Survival; Gefitinib; Glioblastoma; Histone Deacetylase Inhibitors; Humans; Models, Biological; Phenylbutyrates; Piperidines; Protein Kinase Inhibitors; Quinazolines; Receptor Protein-Tyrosine Kinases; Tumor Stem Cell Assay

2011
Antitumour efficacy of MEK inhibitors in human lung cancer cells and their derivatives with acquired resistance to different tyrosine kinase inhibitors.
    British journal of cancer, 2011, Jul-26, Volume: 105, Issue:3

    Topics: Adenocarcinoma; Adenocarcinoma of Lung; Animals; Benzenesulfonates; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; Epithelial-Mesenchymal Transition; Erlotinib Hydrochloride; Gefitinib; Gene Expression Profiling; Humans; Lung Neoplasms; MAP Kinase Kinase Kinases; Mice; Mice, Nude; Niacinamide; Phenylurea Compounds; Piperidines; Protein Kinase Inhibitors; Pyridines; Quinazolines; Sorafenib; Xenograft Model Antitumor Assays

2011
Interaction of the EGFR inhibitors gefitinib, vandetanib, pelitinib and neratinib with the ABCG2 multidrug transporter: implications for the emergence and reversal of cancer drug resistance.
    Biochemical pharmacology, 2012, Aug-01, Volume: 84, Issue:3

    Topics: Aminoquinolines; Aniline Compounds; Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Cell Line; Cell Survival; Drug Resistance, Neoplasm; ErbB Receptors; Gefitinib; Humans; Neoplasm Proteins; Piperidines; Protein Binding; Quinazolines; Quinolines

2012
Identification of CCDC6-RET fusion in the human lung adenocarcinoma cell line, LC-2/ad.
    Journal of thoracic oncology : official publication of the International Association for the Study of Lung Cancer, 2012, Volume: 7, Issue:12

    Topics: Adenocarcinoma; Animals; Antineoplastic Combined Chemotherapy Protocols; Blotting, Western; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Cytoskeletal Proteins; Female; Gefitinib; Humans; Immunoenzyme Techniques; Lung Neoplasms; Mice; Mice, Inbred NOD; Mice, SCID; Oncogene Proteins, Fusion; Phosphorylation; Piperidines; Proto-Oncogene Proteins c-ret; Quinazolines; Real-Time Polymerase Chain Reaction; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Transplantation, Heterologous; Tumor Cells, Cultured

2012
PXR-mediated P-glycoprotein induction by small molecule tyrosine kinase inhibitors.
    European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences, 2013, Mar-12, Volume: 48, Issue:4-5

    Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily B, Member 1; Cell Line, Tumor; Drug Resistance, Neoplasm; Erlotinib Hydrochloride; Gefitinib; Humans; Niacinamide; Phenylurea Compounds; Piperidines; Pregnane X Receptor; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrimidines; Quinazolines; Receptors, Steroid; Sorafenib

2013
Erlotinib, gefitinib, and vandetanib inhibit human nucleoside transporters and protect cancer cells from gemcitabine cytotoxicity.
    Clinical cancer research : an official journal of the American Association for Cancer Research, 2014, Jan-01, Volume: 20, Issue:1

    Topics: Antimetabolites, Antineoplastic; Biological Transport; Cell Line, Tumor; Cell Survival; Deoxycytidine; Drug Screening Assays, Antitumor; Drug Synergism; Erlotinib Hydrochloride; Gefitinib; Gemcitabine; Humans; Inhibitory Concentration 50; Nucleoside Transport Proteins; Piperidines; Quinazolines; Saccharomyces cerevisiae; Uridine

2014
EGF Induced RET Inhibitor Resistance in CCDC6-RET Lung Cancer Cells.
    Yonsei medical journal, 2017, Volume: 58, Issue:1

    Topics: Adenocarcinoma; Cell Line, Tumor; Cetuximab; Drug Resistance, Neoplasm; Epidermal Growth Factor; ErbB Receptors; fms-Like Tyrosine Kinase 3; Gefitinib; Gene Rearrangement; Hepatocyte Growth Factor; Humans; Indoles; Lung Neoplasms; MAP Kinase Signaling System; Mutation; Niacinamide; Phenylurea Compounds; Piperidines; Protein Kinase Inhibitors; Proto-Oncogene Mas; Proto-Oncogene Proteins c-ret; Pyrroles; Quinazolines; RNA, Small Interfering; Signal Transduction; Sorafenib; Sunitinib

2017
Investigation of the binding characteristics between ligands and epidermal growth factor receptor by cell membrane chromatography.
    Journal of molecular recognition : JMR, 2018, Volume: 31, Issue:6

    Topics: Afatinib; Cell Membrane; Chromatography; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; HEK293 Cells; Humans; Ligands; Molecular Docking Simulation; Morpholines; Piperidines; Protein Binding; Protein Kinase Inhibitors; Quinazolines

2018
The ixabepilone and vandetanib combination shows synergistic activity in docetaxel-resistant MDA-MB-231 breast cancer cells.
    Pharmacological reports : PR, 2022, Volume: 74, Issue:5

    Topics: Annexin A5; Antineoplastic Agents; Apoptosis; Caspase 3; Cell Line, Tumor; Cell Proliferation; Cytotoxins; Docetaxel; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Humans; Lapatinib; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-bcl-2; Triple Negative Breast Neoplasms

2022
chemdatabank.com