Compounds > gefitinib
Page last updated: 2024-09-03

gefitinib and erlotinib

gefitinib has been researched along with erlotinib in 72 studies

Compound Research Comparison

Studies
(gefitinib)		Trials
(gefitinib)		Recent Studies (post-2010)
(gefitinib)		Studies
(erlotinib)		Trials
(erlotinib)		Recent Studies (post-2010) (erlotinib)
5,2315662,9192210180

Protein Interaction Comparison

ProteinTaxonomygefitinib (IC50)erlotinib (IC50)
epidermal growth factor receptor isoform a precursorHomo sapiens (human)0.001
Cyclin-G-associated kinaseHomo sapiens (human)0.474
Tyrosine-protein kinase JAK2Homo sapiens (human)4
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)0.55
Bile salt export pumpHomo sapiens (human)10
Proto-oncogene tyrosine-protein kinase SrcGallus gallus (chicken)0.99
Epidermal growth factor receptorHomo sapiens (human)0.5294
Receptor tyrosine-protein kinase erbB-2Homo sapiens (human)0.7171
Cytochrome P450 3A4Homo sapiens (human)0.016
Platelet-derived growth factor receptor betaHomo sapiens (human)0.0122
Serine/threonine-protein kinase B-rafHomo sapiens (human)0.06
Corticosteroid 11-beta-dehydrogenase isozyme 1 Rattus norvegicus (Norway rat)0.03
Platelet-derived growth factor receptor alphaHomo sapiens (human)8.12
Vascular endothelial growth factor receptor 1 Homo sapiens (human)0.25
Receptor tyrosine-protein kinase erbB-3Homo sapiens (human)0.2586
Sodium-dependent dopamine transporterRattus norvegicus (Norway rat)0.369
Cyclin-dependent kinase 2Homo sapiens (human)1.14
Adenosine receptor A1Rattus norvegicus (Norway rat)0.0063
Serine/threonine-protein kinase B-raf Mus musculus (house mouse)0.06
Cytochrome P450 2C19Homo sapiens (human)0.087
Vascular endothelial growth factor receptor 3Homo sapiens (human)0.25
Vascular endothelial growth factor receptor 2Homo sapiens (human)0.8349
D(1A) dopamine receptorSus scrofa (pig)0.3
Fatty-acid amide hydrolase 1Rattus norvegicus (Norway rat)0.0095
Synaptic vesicular amine transporterRattus norvegicus (Norway rat)0.001
Focal adhesion kinase 1Homo sapiens (human)7.4
Receptor tyrosine-protein kinase erbB-4Homo sapiens (human)0.6925
Canalicular multispecific organic anion transporter 1Homo sapiens (human)10
Alpha-1A adrenergic receptor Sus scrofa (pig)0.3
Serine/threonine-protein kinase TBK1Homo sapiens (human)2.2
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)0.13

Research

Studies (72)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's13 (18.06)29.6817
2010's45 (62.50)24.3611
2020's14 (19.44)2.80

Authors

AuthorsStudies
Brawner Floyd, MB; Greenberger, LM; Nilakantan, R; Rabindran, SK; Shen, R; Tsou, HR; Wang, YF; Wissner, A1
Cockerill, S; Guntrip, SB; Lackey, K; Rusnak, D; Smith, K; Vanderwall, D; Wood, E; Zhang, YM1
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
Althaus, IW; Amato, DM; Bridges, AJ; Denny, WA; Elliott, WL; Ellis, PA; Fry, DW; Gonzales, AJ; Han, HK; Harvey, PJ; Klutchko, SR; Meade, MA; Nelson, JM; Pace, G; Roberts, BJ; Sherwood, V; Showalter, HD; Smaill, JB; Tran, TP; Winters, RT; Zhou, H1
Fu, X; Ho, WT; Ishii, T; Li, Q; Li, Z; Xing, S; Xu, M; Zhao, ZJ1
Chen, SF; Liu, HH; Liu, LT; Wu, YT; Yuan, TT1
Löwe, W; Lüth, A1
Bullock, AN; Fedorov, O; Knapp, S; Marsden, B; Müller, S; Pogacic, V; Rellos, P; Schwaller, J; Sundström, M1
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
Artursson, P; Bergström, CA; Hoogstraate, J; Matsson, P; Norinder, U; Pedersen, JM1
Balk, SP; Didonato, M; Flatauer, L; Gray, NS; Hur, W; Jiang, X; Kim, S; Larson, B; Mason, DE; Nagle, A; Peters, EC; Suzuki, M; Valente, D; Velentza, A; Warmuth, M; Zagorska, A; Zhang, J1
Alberti, JG; Alligood, KJ; Caferro, TR; Chamberlain, SD; Dickerson, SH; Dickson, HD; Emerson, HK; Gerding, RM; Griffin, RJ; Hubbard, RD; Keith, BR; Mullin, RJ; Petrov, KG; Reno, MJ; Rheault, TR; Rusnak, DW; Sammond, DM; Smith, SC; Stevens, KL; Uehling, DE; Waterson, AG; Wood, ER1
Bikker, JA; Brooijmans, N; Mansour, TS; Wissner, A1
Ban, HS; Hatori, M; Nabeyama, W; Nakamura, H; Tanaka, Y1
Benfenati, E; Raska, I; Toropov, AA; Toropova, AP1
Morphy, R1
Ji, M; Li, M; Lian, J; Qu, Y; Tang, W; Wu, X; Xu, L; Zheng, Y1
Dohi, K; Haga, N; Iguchi, M; Inoue, M; Matsuo, K; Murashi, T; Ohara, T; Oomori, N; Sentou, J; Shiota, T; Suzuki, N; Wada, T; Watanabe, F; Yari, H1
Hajduk, PJ; Johnson, EF; Kifle, L; Merta, PJ; Metz, JT; Soni, NB1
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
Dohi, K; Haga, N; Iguchi, M; Inoue, M; Matsuo, K; Murashi, T; Ohara, T; Omori, N; Sentou, J; Shiota, T; Suzuki, N; Wada, T; Watanabe, F; Yari, H1
Al-Mazaideh, GM; Erdmann, F; Göllner, C; Rohe, A; Schmidt, M; Sippl, W; Wichapong, K1
Buckley, DB; Funk, RS; Hensley, T; Kazmi, F; Loewen, GJ; Parkinson, A; Pope, C1
Dalvie, D; Loi, CM; Smith, DA1
Cai, J; Chen, J; Ji, M; Sun, M; Wang, P; Wu, X; Zong, X1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Anderton, MJ; Ashton, S; Bethel, PA; Box, M; Butterworth, S; Chorley, CG; Chuaqui, C; Colclough, N; Cross, DA; Dakin, LA; Debreczeni, JÉ; Eberlein, C; Finlay, MR; Grist, M; Hill, GB; Klinowska, TC; Lane, C; Martin, S; Orme, JP; Smith, P; Wang, F; Ward, RA; Waring, MJ1
Chen, X; Du, Y; Kong, L; Sun, H; Sun, M; Wang, F1
Bullock, AN; Canning, P; Choi, S; Cuny, GD; Mohedas, AH; Sanvitale, CE; Wang, Y; Xing, X; Yu, PB1
Chai, S; Ke, CQ; Lin, G; Tang, C; To, KK; Wang, YZ; Yao, S; Ye, Y; Yin, C1
Cheng, W; Hu, Y; Peng, P; Qiu, N; Sheng, R; Yuan, Y1
Bhattacharya, R; Bovonratwet, P; Liu, L; Mathew, MP; Saeui, CT; Tan, E; Yarema, KJ1
Barouch-Bentov, R; Bekerman, E; Chaikuad, A; Chang, L; De Jonghe, S; Einav, S; Herdewijn, P; Heroven, C; Knapp, S; Kovackova, S; Neveu, G; Šála, M1
Abou El Ella, DA; Aly, RM; El-Motwally, AM; Ibrahim, DA1
Chen, K; Cheng, Z; Johnström, P; Li, DY; Varnäs, K; Wang, J; Yang, ZF; Zeng, Q; Zhang, X1
Bantscheff, M; Bergamini, G; Gohlke, B; Gupta, V; Handa, H; Heinzlmeir, S; Helm, D; Klaeger, S; Kuster, B; Médard, G; Perrin, J; Preissner, R; Qiao, H; Savitski, MM1
Hu, L; Li, Z; Liu, P; Lv, Y; Qin, X; Yang, L; Zeng, C1
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K1
Hu, L; Li, Z; Liu, P; Pan, Z; Qin, X; Yang, L; Zeng, C1
Chen, X; Du, Y; Han, J; Sun, H; Sun, M; Wang, F; Zhao, J; Zong, Z1
Fischer, T; Hilgeroth, A; Krüger, T; Najjar, A; Ritter, C; Schächtele, C; Sippl, W; Totzke, F1
Abouzid, KAM; Lasheen, DS; Milik, SN; Serya, RAT1
Chen, ZS; Korlipara, V; Lei, Z; Romu, AA; Zhou, B1
Agarwal, M; Digwal, CS; Pandya, AN; Pandya, DH; Patel, S; Sharma, JA; Vasu, KK1
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
Hou, W; Ma, Y; Ren, Y; Sun, H; Yan, B; Zhang, Z1
Abbas, SY; Ammar, YA; Belal, A; Mehany, ABM; Mohamed, YA; Ragab, A; Sh El-Sharief, AM1
Mathias, F; Montana, M; Terme, T; Vanelle, P1
Guo, Y; He, J; Li, Y; Liu, M; Liu, Y; Xiao, J; Yu, W; Zhang, Q1
Asquith, CRM; Bennett, JM; Berger, BT; Capuzzi, SJ; Crona, DJ; Drewry, DH; Earp, HS; East, MP; Elkins, JM; Fedorov, O; Godoi, PH; Hunter, DM; Knapp, S; Müller, S; Torrice, CD; Wan, J; Wells, CI; Willson, TM; Zuercher, WJ1
Das, D; Hong, J1
Asquith, CRM; Drewry, DH; East, MP; Havener, TM; Johnson, GL; Laitinen, T; Morris, DC; Naegeli, KM; Wells, CI; Zuercher, WJ1
Basetti, V; Keesara, M; Maiti, P; Mansour, TS; Moghudula, AG; Pallepati, RR; Potluri, V1
Asquith, CRM; Treiber, DK; Zuercher, WJ1
Asquith, CRM; Crona, DJ; Fleck, N; Grundner, C; Torrice, CD; Zuercher, WJ1
Abouzid, KAM; Chen, CS; Dokla, EME; Fang, CS1
Jiang, Y; Wu, X; Yan, R; Yang, H; Yang, Z; Zhang, J; Zhang, T; Zhang, X; Zhou, M1
Talele, TT1
Jia, J; Sun, H; Sun, M; Wang, F1
Chen, Y; Cheng, Z; Huang, X; Jiang, Y; Qiao, H; Xie, J; Yang, L; Yu, B; Zhao, W; Zhou, W1
Abd El-Karim, SS; Ahmed, NS; Anwar, MM; El-Hallouty, SM; Srour, AM1
Kargbo, RB1
An, B; Chen, C; Fan, R; Li, J; Li, X; Song, X; Wei, S; Zhang, Q; Zou, Y1
Bharate, SB; Raghuvanshi, R1
Chen, XB; Wang, S; Wang, SQ; Yu, B; Yuan, XH; Zhao, W1
Gou, S; Liu, Q; Liu, Z; Xia, S; Zhang, B1
Aziz, MW; Elgendy, AA; Kamal, AM; Mohamed, KO1
Caballero, E; García-Cárceles, J; Gil, C; Martínez, A1
Cai, Z; Ghaleb, H; Huang, W; Jiang, Y; Liu, Y; Qian, H; Qiu, Q; Shi, W; Yin, Z; Zhang, P; Zhou, J; Zou, F1
Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF1

Reviews

10 review(s) available for gefitinib and erlotinib

ArticleYear
Selectively nonselective kinase inhibition: striking the right balance.
    Journal of medicinal chemistry, 2010, Feb-25, Volume: 53, Issue:4

    Topics: Animals; Antineoplastic Agents; Drug Design; Drug Discovery; Humans; Protein Binding; Protein Kinase Inhibitors; Structure-Activity Relationship

2010
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
    Drug discovery today, 2016, Volume: 21, Issue:4

    Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk

2016
How to train your inhibitor: Design strategies to overcome resistance to Epidermal Growth Factor Receptor inhibitors.
    European journal of medicinal chemistry, 2017, Dec-15, Volume: 142

    Topics: Animals; Antineoplastic Agents; Drug Design; Drug Resistance, Neoplasm; ErbB Receptors; Gene Amplification; Humans; Models, Molecular; Neoplasms; Point Mutation; Protein Domains; Protein Kinase Inhibitors; Receptor, ErbB-2

2017
Antitumoral activity of quinoxaline derivatives: A systematic review.
    European journal of medicinal chemistry, 2019, Feb-01, Volume: 163

    Topics: Antineoplastic Agents; Humans; Neoplasms; Quinoxalines

2019
The association between anti-tumor potency and structure-activity of protein-kinases inhibitors based on quinazoline molecular skeleton.
    Bioorganic & medicinal chemistry, 2019, 02-01, Volume: 27, Issue:3

    Topics: Animals; Antineoplastic Agents; Cell Proliferation; Humans; Neoplasms; Protein Kinase Inhibitors; Protein Kinases; Quinazolines

2019
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
Design, synthesis and biological evaluation of 2-amino-4-(1,2,4-triazol)pyridine derivatives as potent EGFR inhibitors to overcome TKI-resistance.
    European journal of medicinal chemistry, 2020, Feb-01, Volume: 187

    Topics: Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Drug Design; ErbB Receptors; Humans; Protein Kinase Inhibitors; Pyridines

2020
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

Other Studies

62 other study(ies) available for gefitinib and erlotinib

ArticleYear
Syntheses and EGFR and HER-2 kinase inhibitory activities of 4-anilinoquinoline-3-carbonitriles: analogues of three important 4-anilinoquinazolines currently undergoing clinical evaluation as therapeutic antitumor agents.
    Bioorganic & medicinal chemistry letters, 2002, Oct-21, Volume: 12, Issue:20

    Topics: Antineoplastic Agents; Cell Line; Cyclization; Enzyme Inhibitors; ErbB Receptors; Magnetic Resonance Spectroscopy; Mass Spectrometry; Models, Molecular; Molecular Conformation; Nitriles; Quinolines; Receptor, ErbB-2

2002
Synthesis and SAR of potent EGFR/erbB2 dual inhibitors.
    Bioorganic & medicinal chemistry letters, 2004, Jan-05, Volume: 14, Issue:1

    Topics: Binding Sites; Cell Line, Tumor; Enzyme Inhibitors; ErbB Receptors; Glycoproteins; Humans; Receptor, ErbB-2; Structure-Activity Relationship

2004
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
Tyrosine kinase inhibitors. 19. 6-Alkynamides of 4-anilinoquinazolines and 4-anilinopyrido[3,4-d]pyrimidines as irreversible inhibitors of the erbB family of tyrosine kinase receptors.
    Journal of medicinal chemistry, 2006, Feb-23, Volume: 49, Issue:4

    Topics: Alkynes; Amides; Aniline Compounds; Animals; Antineoplastic Agents; Cell Line; Dogs; ErbB Receptors; Haplorhini; Humans; Mice; Mice, Nude; Mice, SCID; Phosphorylation; Pyrimidines; Quinazolines; Rats; Receptor Protein-Tyrosine Kinases; Receptor, ErbB-2; Receptor, ErbB-4; Structure-Activity Relationship; Xenograft Model Antitumor Assays

2006
Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth.
    The Journal of biological chemistry, 2007, Feb-09, Volume: 282, Issue:6

    Topics: Amino Acid Substitution; Animals; Cell Line, Tumor; Cell Proliferation; Drug Delivery Systems; Enzyme Activation; Erlotinib Hydrochloride; Growth Inhibitors; Hematopoietic Stem Cells; Humans; Janus Kinase 2; Jurkat Cells; Mice; Phenylalanine; Polycythemia Vera; Protein Kinase Inhibitors; Quinazolines; Valine

2007
Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors.
    Bioorganic & medicinal chemistry letters, 2007, Nov-15, Volume: 17, Issue:22

    Topics: Aniline Compounds; Antineoplastic Agents; Computer Simulation; Drug Screening Assays, Antitumor; ErbB Receptors; Inhibitory Concentration 50; Models, Molecular; Molecular Structure; Quinazolines; Structure-Activity Relationship

2007
Syntheses of 4-(indole-3-yl)quinazolines: a new class of epidermal growth factor receptor tyrosine kinase inhibitors.
    European journal of medicinal chemistry, 2008, Volume: 43, Issue:7

    Topics: Cell Line, Tumor; ErbB Receptors; Humans; Magnetic Resonance Spectroscopy; Mass Spectrometry; Protein Kinase Inhibitors; Quinazolines

2008
A systematic interaction map of validated kinase inhibitors with Ser/Thr kinases.
    Proceedings of the National Academy of Sciences of the United States of America, 2007, Dec-18, Volume: 104, Issue:51

    Topics: Amino Acid Sequence; Binding Sites; Clinical Trials as Topic; Drug Evaluation, Preclinical; Enzyme Stability; Humans; Molecular Sequence Data; Phylogeny; Protein Array Analysis; Protein Conformation; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases

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
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
    Journal of medicinal chemistry, 2008, Jun-12, Volume: 51, Issue:11

    Topics: Administration, Oral; Animals; Antineoplastic Agents; Antipsychotic Agents; Antiviral Agents; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Biological Transport; Cell Line; Computer Simulation; Cytochrome P-450 Enzyme System; Drug-Related Side Effects and Adverse Reactions; Estradiol; Humans; Insecta; Liver; Models, Molecular; Multidrug Resistance-Associated Protein 2; Multidrug Resistance-Associated Proteins; Neoplasm Proteins; Pharmaceutical Preparations; Pharmacology; Structure-Activity Relationship

2008
Clinical stage EGFR inhibitors irreversibly alkylate Bmx kinase.
    Bioorganic & medicinal chemistry letters, 2008, Nov-15, Volume: 18, Issue:22

    Topics: Animals; Cysteine; ErbB Receptors; Mice; Molecular Structure; Morpholines; Protein-Tyrosine Kinases; Quinazolines; Sequence Homology, Amino Acid

2008
Synthesis and stereochemical effects of pyrrolidinyl-acetylenic thieno[3,2-d]pyrimidines as EGFR and ErbB-2 inhibitors.
    Bioorganic & medicinal chemistry letters, 2009, Jan-01, Volume: 19, Issue:1

    Topics: Administration, Oral; Animals; Antineoplastic Agents; ErbB Receptors; Mice; Pharmacokinetics; Pyrimidines; Pyrrolidines; Receptor, ErbB-2; Structure-Activity Relationship

2009
Kinase domain mutations in cancer: implications for small molecule drug design strategies.
    Journal of medicinal chemistry, 2009, Mar-26, Volume: 52, Issue:6

    Topics: Amino Acid Sequence; Antineoplastic Agents; Drug Design; Enzyme Inhibitors; Humans; Molecular Sequence Data; Mutation; Neoplasms; Phosphotransferases; Protein Conformation

2009
Enhancement of EGFR tyrosine kinase inhibition by C-C multiple bonds-containing anilinoquinazolines.
    Bioorganic & medicinal chemistry, 2010, Jan-15, Volume: 18, Issue:2

    Topics: Aniline Compounds; Antineoplastic Agents; Apoptosis; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Immunoblotting; Molecular Structure; Protein Kinase Inhibitors; Quinazolines; Stereoisomerism; Structure-Activity Relationship

2010
QSPR modeling of octanol/water partition coefficient of antineoplastic agents by balance of correlations.
    European journal of medicinal chemistry, 2010, Volume: 45, Issue:4

    Topics: Antineoplastic Agents; Models, Chemical; Octanols; Quantitative Structure-Activity Relationship; Water

2010
Design and synthesis of novel Gefitinib analogues with improved anti-tumor activity.
    Bioorganic & medicinal chemistry, 2010, Jun-01, Volume: 18, Issue:11

    Topics: Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Drug Design; ErbB Receptors; Gefitinib; Humans; Quinazolines; Receptor, ErbB-2

2010
Synthesis and evaluation of novel pyrimidine-based dual EGFR/Her-2 inhibitors.
    Bioorganic & medicinal chemistry letters, 2011, Mar-15, Volume: 21, Issue:6

    Topics: Crystallography, X-Ray; Drug Evaluation, Preclinical; ErbB Receptors; Humans; Models, Molecular; Pyrimidines; Receptor, ErbB-2; Structure-Activity Relationship

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

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

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
Discovery of novel 5-alkynyl-4-anilinopyrimidines as potent, orally active dual inhibitors of EGFR and Her-2 tyrosine kinases.
    Bioorganic & medicinal chemistry letters, 2012, Jan-01, Volume: 22, Issue:1

    Topics: Administration, Oral; Animals; Chemistry, Pharmaceutical; Drug Design; Drug Screening Assays, Antitumor; Enzyme Inhibitors; ErbB Receptors; Humans; Hydrogen-Ion Concentration; Inhibitory Concentration 50; Mice; Microsomes, Liver; Models, Chemical; Neoplasm Transplantation; Pyrimidines; Rats; Receptor, ErbB-2; Structure-Activity Relationship

2012
Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay.
    European journal of medicinal chemistry, 2013, Volume: 61

    Topics: Dose-Response Relationship, Drug; Fluorescence Resonance Energy Transfer; Glycolipids; Humans; Membrane Proteins; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Structure-Activity Relationship

2013
Lysosomal sequestration (trapping) of lipophilic amine (cationic amphiphilic) drugs in immortalized human hepatocytes (Fa2N-4 cells).
    Drug metabolism and disposition: the biological fate of chemicals, 2013, Volume: 41, Issue:4

    Topics: Adrenergic beta-Antagonists; Amines; Ammonium Chloride; Antidepressive Agents, Tricyclic; Atorvastatin; Cell Line, Transformed; Diuretics; Hepatocytes; Heptanoic Acids; Humans; Hydroxymethylglutaryl-CoA Reductase Inhibitors; Imipramine; Lysosomes; Monensin; Nigericin; Propranolol; Pyrroles

2013
Which metabolites circulate?
    Drug metabolism and disposition: the biological fate of chemicals, 2013, Volume: 41, Issue:5

    Topics: Humans; Metabolic Clearance Rate; Pharmaceutical Preparations

2013
Design and synthesis of novel 4-benzothiazole amino quinazolines Dasatinib derivatives as potential anti-tumor agents.
    European journal of medicinal chemistry, 2013, Volume: 63

    Topics: Antineoplastic Agents; Benzothiazoles; Cell Line, Tumor; Cell Proliferation; Cell Survival; Dasatinib; Dose-Response Relationship, Drug; Drug Design; HCT116 Cells; Humans; Inhibitory Concentration 50; K562 Cells; Models, Chemical; Molecular Structure; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-abl; Pyrimidines; Quinazolines; src-Family Kinases; Thiazoles; U937 Cells

2013
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
Structure- and reactivity-based development of covalent inhibitors of the activating and gatekeeper mutant forms of the epidermal growth factor receptor (EGFR).
    Journal of medicinal chemistry, 2013, Sep-12, Volume: 56, Issue:17

    Topics: ErbB Receptors; Models, Molecular; Mutation; Structure-Activity Relationship

2013
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 1: erlotinib analogs.
    Bioorganic & medicinal chemistry letters, 2014, Feb-01, Volume: 24, Issue:3

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cyclization; Enzyme Activation; ErbB Receptors; Erlotinib Hydrochloride; Humans; Inhibitory Concentration 50; Molecular Structure; Oxazepines; Oxazines; Phosphotransferases; Protein Binding; Quinazolines; Receptor, ErbB-2

2014
Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
    Journal of medicinal chemistry, 2014, Oct-09, Volume: 57, Issue:19

    Topics: Activin Receptors, Type I; Aminopyridines; Humans; Mutation; Myositis Ossificans; Phenols; Protein Kinase Inhibitors; Structure-Activity Relationship

2014
Polyoxypregnane steroids from the stems of Marsdenia tenacissima.
    Journal of natural products, 2014, Sep-26, Volume: 77, Issue:9

    Topics: Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Erlotinib Hydrochloride; Gefitinib; Glycosides; Humans; Marsdenia; Molecular Structure; Nuclear Magnetic Resonance, Biomolecular; Pregnanes; Quinazolines

2014
Identification of novel 4-anilinoquinazoline derivatives as potent EGFR inhibitors both under normoxia and hypoxia.
    Bioorganic & medicinal chemistry, 2014, Dec-15, Volume: 22, Issue:24

    Topics: Aniline Compounds; Antineoplastic Agents; Apoptosis; Binding Sites; Cell Hypoxia; Cell Line, Tumor; Cell Proliferation; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; HT29 Cells; Humans; Molecular Docking Simulation; NADP; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Quinazolines; Structure-Activity Relationship

2014
Metabolic glycoengineering sensitizes drug-resistant pancreatic cancer cells to tyrosine kinase inhibitors erlotinib and gefitinib.
    Bioorganic & medicinal chemistry letters, 2015, Mar-15, Volume: 25, Issue:6

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Drug Resistance, Neoplasm; Drug Synergism; ErbB Receptors; Erlotinib Hydrochloride; Gefitinib; Glycosylation; Humans; Metabolic Engineering; Pancreatic Neoplasms; Phosphorylation; Protein Kinase Inhibitors; Quinazolines; STAT Transcription Factors

2015
Selective Inhibitors of Cyclin G Associated Kinase (GAK) as Anti-Hepatitis C Agents.
    Journal of medicinal chemistry, 2015, Apr-23, Volume: 58, Issue:8

    Topics: Antiviral Agents; Cell Line; Crystallography, X-Ray; Hepacivirus; Hepatitis C; Humans; Intracellular Signaling Peptides and Proteins; Models, Molecular; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pyridines; Thiazoles; Virus Internalization

2015
Molecular design and synthesis of certain new quinoline derivatives having potential anticancer activity.
    European journal of medicinal chemistry, 2015, Sep-18, Volume: 102

    Topics: Antineoplastic Agents; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; MCF-7 Cells; Molecular Structure; Protein Kinase Inhibitors; Quinolines; Structure-Activity Relationship

2015
Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor.
    Journal of medicinal chemistry, 2015, Oct-22, Volume: 58, Issue:20

    Topics: Animals; Brain; Brain Neoplasms; Central Nervous System; Clinical Trials, Phase I as Topic; Dogs; Drug Discovery; ErbB Receptors; Macaca fascicularis; Male; Mice; Piperazines; Positron-Emission Tomography; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Quinazolines; Rats; Rats, Wistar; Xenograft Model Antitumor Assays

2015
Chemical Proteomics Reveals Ferrochelatase as a Common Off-target of Kinase Inhibitors.
    ACS chemical biology, 2016, 05-20, Volume: 11, Issue:5

    Topics: Benzocycloheptenes; Cell Line, Tumor; Ferrochelatase; Heme; Humans; Imidazoles; Indoles; Molecular Docking Simulation; Protein Binding; Protein Kinase Inhibitors; Proteomics; Pyrazines; Pyridines; Quinolines; Sulfonamides; Vemurafenib

2016
Novel morpholin-3-one fused quinazoline derivatives as EGFR tyrosine kinase inhibitors.
    Bioorganic & medicinal chemistry letters, 2016, Mar-15, Volume: 26, Issue:6

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Molecular Docking Simulation; Molecular Structure; Morpholines; Protein Kinase Inhibitors; Quinazolines; Structure-Activity Relationship

2016
Discovery of new [1,4]dioxino[2,3-f]quinazoline-based inhibitors of EGFR including the T790M/L858R mutant.
    Bioorganic & medicinal chemistry, 2016, 07-01, Volume: 24, Issue:13

    Topics: A549 Cells; Antineoplastic Agents; Cell Proliferation; Drug Discovery; ErbB Receptors; Humans; Inhibitory Concentration 50; Lung Neoplasms; Molecular Structure; Mutation; Protein Binding; Quinazolines

2016
Synthesis and biological evaluation of novel tricyclic oxazine and oxazepine fused quinazolines. Part 2: Gefitinib analogs.
    Bioorganic & medicinal chemistry letters, 2016, 10-01, Volume: 26, Issue:19

    Topics: Cell Line; ErbB Receptors; Gefitinib; Humans; Phosphorylation; Quinazolines

2016
Discovery of novel substituted benzo-anellated 4-benzylamino pyrrolopyrimidines as dual EGFR and VEGFR2 inhibitors.
    Bioorganic & medicinal chemistry letters, 2017, 06-15, Volume: 27, Issue:12

    Topics: Antineoplastic Agents; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Molecular Docking Simulation; Molecular Structure; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Structure-Activity Relationship; Vascular Endothelial Growth Factor Receptor-2

2017
Design, synthesis and biological evaluation of WZ4002 analogues as EGFR inhibitors.
    Bioorganic & medicinal chemistry letters, 2017, 11-01, Volume: 27, Issue:21

    Topics: Acrylamides; Animals; Cell Line, Tumor; Cell Survival; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Mice; Mutagenesis, Site-Directed; Protein Kinase Inhibitors; Pyrimidines; Structure-Activity Relationship

2017
Imidazo[1,2-a]pyridines linked with thiazoles/thiophene motif through keto spacer as potential cytotoxic agents and NF-κB inhibitors.
    Bioorganic & medicinal chemistry letters, 2017, 12-15, Volume: 27, Issue:24

    Topics: A549 Cells; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Drug Screening Assays, Antitumor; HeLa Cells; Humans; NF-kappa B; Pyridines; Structure-Activity Relationship; Thiazoles; Thiophenes

2017
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
Novel quinazoline derivatives bearing various 6-benzamide moieties as highly selective and potent EGFR inhibitors.
    Bioorganic & medicinal chemistry, 2018, 05-01, Volume: 26, Issue:8

    Topics: Antineoplastic Agents; Benzamides; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Molecular Structure; Protein Kinase Inhibitors; Quinazolines; Structure-Activity Relationship; Tumor Cells, Cultured

2018
Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity.
    European journal of medicinal chemistry, 2018, Aug-05, Volume: 156

    Topics: Antineoplastic Agents; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Isatin; Molecular Docking Simulation; Neoplasms; Protein Kinase Inhibitors

2018
SGC-GAK-1: A Chemical Probe for Cyclin G Associated Kinase (GAK).
    Journal of medicinal chemistry, 2019, 03-14, Volume: 62, Issue:5

    Topics: Cyclin G; HEK293 Cells; Humans; Intracellular Signaling Peptides and Proteins; Male; Molecular Probes; Protein Serine-Threonine Kinases

2019
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
Lead generation of 1,2-dithiolanes as exon 19 and exon 21 mutant EGFR tyrosine kinase inhibitors.
    Bioorganic & medicinal chemistry letters, 2019, 06-15, Volume: 29, Issue:12

    Topics: Exons; Humans; Mutation; Protein Kinase Inhibitors; Thioctic Acid

2019
Utilizing comprehensive and mini-kinome panels to optimize the selectivity of quinoline inhibitors for cyclin G associated kinase (GAK).
    Bioorganic & medicinal chemistry letters, 2019, 07-15, Volume: 29, Issue:14

    Topics: Cyclin G; Humans; Protein Kinase Inhibitors; Quinolines

2019
Anti-tubercular activity of novel 4-anilinoquinolines and 4-anilinoquinazolines.
    Bioorganic & medicinal chemistry letters, 2019, 09-15, Volume: 29, Issue:18

    Topics: Aniline Compounds; Antitubercular Agents; Dose-Response Relationship, Drug; Microbial Sensitivity Tests; Molecular Structure; Mycobacterium tuberculosis; Quinazolines; Quinolines; Structure-Activity Relationship

2019
1,2,4-Oxadiazole derivatives targeting EGFR and c-Met degradation in TKI resistant NSCLC.
    European journal of medicinal chemistry, 2019, Nov-15, Volume: 182

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Down-Regulation; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Molecular Structure; Oxadiazoles; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-met; Structure-Activity Relationship

2019
Acetylene Group, Friend or Foe in Medicinal Chemistry.
    Journal of medicinal chemistry, 2020, 06-11, Volume: 63, Issue:11

    Topics: Acetylene; Alkynes; Animals; Anti-Inflammatory Agents; Chemistry, Pharmaceutical; Click Chemistry; Half-Life; HIV Reverse Transcriptase; HIV-1; Humans; Macrophages; Mice; Protein Kinase Inhibitors; Rats; Reverse Transcriptase Inhibitors

2020
Design and synthesis of a novel class EGFR/HER2 dual inhibitors containing tricyclic oxazine fused quinazolines scaffold.
    Bioorganic & medicinal chemistry letters, 2020, 05-01, Volume: 30, Issue:9

    Topics: Antineoplastic Agents; Cell Line, Tumor; Drug Design; ErbB Receptors; Humans; Inhibitory Concentration 50; Quinazolines; Receptor, ErbB-2; Structure-Activity Relationship

2020
Discovery of new thieno[3,2-d]pyrimidine derivatives targeting EGFR
    European journal of medicinal chemistry, 2020, Aug-01, Volume: 199

    Topics: Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Cell Survival; Cells, Cultured; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Lung Neoplasms; Molecular Conformation; Molecular Docking Simulation; Protein Kinase Inhibitors; Pyrimidines; Structure-Activity Relationship

2020
Design, synthesis, biological evaluation, QSAR analysis and molecular modelling of new thiazol-benzimidazoles as EGFR inhibitors.
    Bioorganic & medicinal chemistry, 2020, 09-15, Volume: 28, Issue:18

    Topics: Antineoplastic Agents; Apoptosis; Benzimidazoles; Breast Neoplasms; Cell Proliferation; Drug Screening Assays, Antitumor; ErbB Receptors; Erlotinib Hydrochloride; Female; Humans; MCF-7 Cells; Molecular Docking Simulation; Protein Kinase Inhibitors; Quantitative Structure-Activity Relationship; Thiazoles

2020
Complete Regression of Carcinoma via Combined C-RAF and EGFR Targeted Therapy.
    ACS medicinal chemistry letters, 2020, Oct-08, Volume: 11, Issue:10

    Topics:

2020
Design, synthesis and biological evaluation of novel 2,4-diaryl pyrimidine derivatives as selective EGFR
    European journal of medicinal chemistry, 2021, Feb-15, Volume: 212

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; ErbB Receptors; Humans; Male; Mice; Mice, Nude; Models, Molecular; Molecular Structure; Neoplasms, Experimental; Protein Kinase Inhibitors; Pyrimidines; Rats; Rats, Sprague-Dawley; Structure-Activity Relationship

2021
Recent Developments in the Use of Kinase Inhibitors for Management of Viral Infections.
    Journal of medicinal chemistry, 2022, 01-27, Volume: 65, Issue:2

    Topics: Antiviral Agents; COVID-19; COVID-19 Drug Treatment; Drug Approval; Drug Repositioning; High-Throughput Screening Assays; Humans; Protein Kinase Inhibitors; SARS-CoV-2; United States; United States Food and Drug Administration; Virus Diseases

2022
Design, synthesis and biological evaluation of sulfamoylphenyl-quinazoline derivatives as potential EGFR/CAIX dual inhibitors.
    European journal of medicinal chemistry, 2021, Apr-15, Volume: 216

    Topics: Antineoplastic Agents; Apoptosis; Binding Sites; Carbonic Anhydrase IX; Cell Cycle Checkpoints; Cell Line, Tumor; Cell Movement; Cell Proliferation; Down-Regulation; Drug Design; Enzyme Inhibitors; ErbB Receptors; Humans; Molecular Docking Simulation; Protein Kinase Inhibitors; Quinazolines; Structure-Activity Relationship

2021
Design, synthesis and assessment of new series of quinazolinone derivatives as EGFR inhibitors along with their cytotoxic evaluation against MCF7 and A549 cancer cell lines.
    Bioorganic & medicinal chemistry letters, 2021, 06-01, Volume: 41

    Topics: A549 Cells; Antineoplastic Agents; Apoptosis; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; MCF-7 Cells; Molecular Structure; Protein Kinase Inhibitors; Quinazolinones; Structure-Activity Relationship

2021
Exploration of novel phthalazinone derivatives as potential efflux transporter inhibitors for reversing multidrug resistance and improving the oral absorption of paclitaxel.
    European journal of medicinal chemistry, 2022, Apr-05, Volume: 233

    Topics: ATP Binding Cassette Transporter, Subfamily G, Member 2; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Humans; Neoplasm Proteins; Neoplasms; Paclitaxel

2022