Page last updated: 2024-09-05

lapatinib and erlotinib

lapatinib has been researched along with erlotinib in 41 studies

Compound Research Comparison

Studies
(lapatinib)
Trials
(lapatinib)
Recent Studies (post-2010)
(lapatinib)
Studies
(erlotinib)
Trials
(erlotinib)
Recent Studies (post-2010) (erlotinib)
1,9193051,4422210180

Protein Interaction Comparison

ProteinTaxonomylapatinib (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 (41)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (9.76)29.6817
2010's29 (70.73)24.3611
2020's8 (19.51)2.80

Authors

AuthorsStudies
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
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
Cha, MY; Kim, JW; Kim, MS; Kim, YH; Lee, CG; Lee, GS; Lee, KO; Park, SB; Song, JY1
Bao, R; Cai, X; Forrester, J; Lai, CJ; Qian, C; Qu, H; Wang, J; Yin, L; Zhai, HX1
Morphy, R1
Bamaung, NY; Bell, RL; Clark, RF; Davidsen, SK; Erickson, SA; Fidanze, SD; Hubbard, RD; Johnson, EF; Kovar, P; Mantei, R; Pappano, WN; Sheppard, GS; Sorensen, BK; Stewart, KD; Swinger, KK; Tucker, LA; Wang, GT; Wang, J; Wilsbacher, JL; Zhang, Q1
Bell, RL; Bouska, J; Davidsen, SK; Hu, X; Hubbard, RD; Johnson, EF; Kovar, P; Mantei, RA; Osterling, DJ; Sheppard, GS; Tucker, L; Wang, GT; Wang, J; Wilsbacher, JL; Zhang, Q1
Hajduk, PJ; Johnson, EF; Kifle, L; Merta, PJ; Metz, JT; Soni, NB1
Russu, WA; Shallal, HM1
Aertgeerts, K; Habuka, N; Hirokawa, A; Ishikawa, T; Iwamoto, K; Jennings, A; Miki, H; Ohta, Y; Sang, BC; Skene, R; Snell, G; Sogabe, S; Tanaka, T; Yano, J; Zou, H1
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
Beckers, T; Böhmer, FD; Eichhorn, E; Fiebig, HH; Kelter, G; Krumbach, R; Mahboobi, S; Pongratz, H; Schächtele, C; Sellmer, A; Totzke, F1
Ballard, TE; Henderson, JL; Kalgutkar, AS; Obach, RS; Orr, ST; Ripp, SL; Scott, DO; Sun, H1
Al-Mazaideh, GM; Erdmann, F; Göllner, C; Rohe, A; Schmidt, M; Sippl, W; Wichapong, K1
Cantin, LD; Chen, H; Kenna, JG; Noeske, T; Stahl, S; Walker, CL; Warner, DJ1
Buckley, DB; Funk, RS; Hensley, T; Kazmi, F; Loewen, GJ; Parkinson, A; Pope, C1
Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ1
Bailey-Downs, LC; Bastian, A; Disch, BC; Dybdal-Hargreaves, NF; Gangjee, A; Hamel, E; Ihnat, M; Mooberry, SL; Raghavan, S; Rohena, CC; Thorpe, JE; Zhang, X1
Bullock, AN; Canning, P; Choi, S; Cuny, GD; Mohedas, AH; Sanvitale, CE; Wang, Y; Xing, X; Yu, PB1
Abou El Ella, DA; Aly, RM; El-Motwally, AM; Ibrahim, DA1
Chen, LW; Duan, YT; Tang, DJ; Tao, XX; Wang, PF; Xu, C; Yang, MR; Zhu, HL1
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K1
Abouzid, KAM; Lasheen, DS; Milik, SN; Serya, RAT1
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
Abbas, SY; Ammar, YA; Belal, A; Mehany, ABM; Mohamed, YA; Ragab, A; Sh El-Sharief, AM1
Guo, Y; He, J; Li, Y; Liu, M; Liu, Y; Xiao, J; Yu, W; Zhang, Q1
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; Crona, DJ; Fleck, N; Grundner, C; Torrice, CD; Zuercher, WJ1
Liu, Y; Xu, Z; Zhao, SJ1
Jia, J; Sun, H; Sun, M; Wang, F1
Abbas, SY; Al-Harbi, RAK; Sh El-Sharief, MAM1
Abd El-Karim, SS; Ahmed, NS; Anwar, MM; El-Hallouty, SM; Srour, AM1
Baufeld, L; Chow, K; Clark, PM; Cloughesy, TF; Faull, K; Jung, ME; Kim, G; Nathanson, DA; Tsang, JE; Urner, LM1
Abuo-Rahma, GEA; Badr, M; Bass, AKA; El-Zoghbi, MS; Mohamed, MFA; Nageeb, EM1
Chen, XB; Wang, S; Wang, SQ; Yu, B; Yuan, XH; Zhao, W1
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 lapatinib 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
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
    Journal of medicinal chemistry, 2012, Jun-14, Volume: 55, Issue:11

    Topics: Animals; Apoproteins; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Discovery; Drug Interactions; Heme; Humans; Models, Biological; Pharmacokinetics; Structure-Activity Relationship; Time Factors

2012
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
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
1,2,3-Triazole-containing hybrids as potential anticancer agents: Current developments, action mechanisms and structure-activity relationships.
    European journal of medicinal chemistry, 2019, Dec-01, Volume: 183

    Topics: Antineoplastic Agents; Humans; Molecular Structure; Neoplasms; Structure-Activity Relationship; Triazoles

2019
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
    European journal of medicinal chemistry, 2021, Jan-01, Volume: 209

    Topics: Androgen Antagonists; Animals; Antineoplastic Agents; Benzimidazoles; Cyclic Nucleotide Phosphodiesterases, Type 5; Daunorubicin; Doxorubicin; fms-Like Tyrosine Kinase 3; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Molecular Targeted Therapy; Morpholines; Nicotinamide Phosphoribosyltransferase; Nitric Oxide; Pyrimidines; Quinazolines; Structure-Activity Relationship; Transcription Factors

2021
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
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

31 other study(ies) available for lapatinib and erlotinib

ArticleYear
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
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
Discovery of a novel Her-1/Her-2 dual tyrosine kinase inhibitor for the treatment of Her-1 selective inhibitor-resistant non-small cell lung cancer.
    Journal of medicinal chemistry, 2009, Nov-12, Volume: 52, Issue:21

    Topics: Aniline Compounds; Animals; Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Line, Tumor; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; ErbB Receptors; Erlotinib Hydrochloride; Female; Gefitinib; Humans; Lung Neoplasms; Male; Mice; Mice, Nude; Molecular Conformation; Neoplasm Transplantation; Pyrrolidines; Quinazolines; Rats; Receptor, ErbB-2; Stereoisomerism; Structure-Activity Relationship; Transplantation, Heterologous

2009
Discovery of 7-(4-(3-ethynylphenylamino)-7-methoxyquinazolin-6-yloxy)-N-hydroxyheptanamide (CUDc-101) as a potent multi-acting HDAC, EGFR, and HER2 inhibitor for the treatment of cancer.
    Journal of medicinal chemistry, 2010, Mar-11, Volume: 53, Issue:5

    Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Growth Processes; Enzyme Inhibitors; ErbB Receptors; Female; HeLa Cells; Hep G2 Cells; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Mice; Mice, Nude; Neoplasms; Quinazolines; Receptor, ErbB-2; Structure-Activity Relationship; Xenograft Model Antitumor Assays

2010
Imidazo[2,1-b]thiazoles: multitargeted inhibitors of both the insulin-like growth factor receptor and members of the epidermal growth factor family of receptor tyrosine kinases.
    Bioorganic & medicinal chemistry letters, 2010, Apr-15, Volume: 20, Issue:8

    Topics: ErbB Receptors; Models, Molecular; Protein Kinase Inhibitors; Receptor Protein-Tyrosine Kinases; Structure-Activity Relationship; Thiazoles

2010
Substituted 4-amino-1H-pyrazolo[3,4-d]pyrimidines as multi-targeted inhibitors of insulin-like growth factor-1 receptor (IGF1R) and members of ErbB-family receptor kinases.
    Bioorganic & medicinal chemistry letters, 2010, Oct-15, Volume: 20, Issue:20

    Topics: Adenine; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; ErbB Receptors; Humans; Mice; Mice, Inbred C57BL; Neoplasms; Rats; Receptor, ErbB-2; Receptor, IGF Type 1; 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
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
Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein.
    The Journal of biological chemistry, 2011, May-27, Volume: 286, Issue:21

    Topics: Allosteric Regulation; Antineoplastic Agents; Crystallography, X-Ray; Drug Design; Enzyme Activation; ErbB Receptors; Humans; Neoplasms; Protein Kinase Inhibitors; Protein Structure, Tertiary; Receptor, ErbB-2; Receptor, ErbB-4; 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
Novel inhibitors of epidermal growth factor receptor: (4-(Arylamino)-7H-pyrrolo[2,3-d]pyrimidin-6-yl)(1H-indol-2-yl)methanones and (1H-indol-2-yl)(4-(phenylamino)thieno[2,3-d]pyrimidin-6-yl)methanones.
    Bioorganic & medicinal chemistry, 2012, Jan-01, Volume: 20, Issue:1

    Topics: Antineoplastic Agents; Cell Line, Tumor; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Indoles; Phosphorylation; Pyrimidines; Quinazolines; 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
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
    Drug metabolism and disposition: the biological fate of chemicals, 2012, Volume: 40, Issue:12

    Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Bile Acids and Salts; Cell Line; Chemical and Drug Induced Liver Injury; Humans; Quantitative Structure-Activity Relationship

2012
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
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 design and discovery of water soluble 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multitargeted receptor tyrosine kinase inhibitors and microtubule targeting antitumor agents.
    Bioorganic & medicinal chemistry, 2014, Jul-15, Volume: 22, Issue:14

    Topics: Aniline Compounds; Animals; Antineoplastic Agents; Apoptosis; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Female; HeLa Cells; Humans; Mice; Mice, Inbred BALB C; Mice, Nude; Microtubules; Neoplasms, Experimental; Protein Kinase Inhibitors; Pyrimidines; Receptor Protein-Tyrosine Kinases; Solubility; Structure-Activity Relationship; Water

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
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
Design, synthesis and biological evaluation of pyrazolyl-nitroimidazole derivatives as potential EGFR/HER-2 kinase inhibitors.
    Bioorganic & medicinal chemistry letters, 2016, Jan-15, Volume: 26, Issue:2

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Drug Design; ErbB Receptors; Humans; Molecular Docking Simulation; Neoplasms; Nitroimidazoles; Protein Kinase Inhibitors; Pyrazoles; Receptor, ErbB-2

2016
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, 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
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
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
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
Synthesis and anticancer activity of thiourea derivatives bearing a benzodioxole moiety with EGFR inhibitory activity, apoptosis assay and molecular docking study.
    European journal of medicinal chemistry, 2020, Jul-15, Volume: 198

    Topics: Amines; Antineoplastic Agents; Apoptosis; bcl-2-Associated X Protein; Benzodioxoles; Cell Line, Tumor; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Hydrazines; Molecular Docking Simulation; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-bcl-2; Structure-Activity Relationship; Thiosemicarbazones; Thiourea

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
Development of a Potent Brain-Penetrant EGFR Tyrosine Kinase Inhibitor against Malignant Brain Tumors.
    ACS medicinal chemistry letters, 2020, Oct-08, Volume: 11, Issue:10

    Topics:

2020
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