Page last updated: 2024-09-05

erlotinib and su 11248

erlotinib has been researched along with su 11248 in 36 studies

Compound Research Comparison

Studies
(erlotinib)
Trials
(erlotinib)
Recent Studies (post-2010)
(erlotinib)
Studies
(su 11248)
Trials
(su 11248)
Recent Studies (post-2010) (su 11248)
22101804,3385603,200

Protein Interaction Comparison

ProteinTaxonomyerlotinib (IC50)su 11248 (IC50)
Serine/threonine-protein kinase Chk1Homo sapiens (human)0.0773
Aurora kinase AHomo sapiens (human)1.837
Solute carrier family 22 member 1 Homo sapiens (human)6.1
NUAK family SNF1-like kinase 1Homo sapiens (human)0.048
Serine/threonine-protein kinase PAK 4Homo sapiens (human)0.5692
Serine/threonine-protein kinase Chk2Homo sapiens (human)0.0168
Tyrosine-protein kinase ABL1Homo sapiens (human)0.8423
Proto-oncogene tyrosine-protein kinase SrcGallus gallus (chicken)0.555
Epidermal growth factor receptorHomo sapiens (human)0.48
Platelet-derived growth factor receptor betaMus musculus (house mouse)0.0186
Insulin receptorHomo sapiens (human)3.2
Tyrosine-protein kinase LckHomo sapiens (human)0.0089
Macrophage colony-stimulating factor 1 receptorHomo sapiens (human)0.0888
Proto-oncogene tyrosine-protein kinase receptor RetHomo sapiens (human)0.35
Hepatocyte growth factor receptorHomo sapiens (human)4.0002
Tyrosine-protein kinase HCKHomo sapiens (human)0.19
Platelet-derived growth factor receptor betaHomo sapiens (human)0.211
Mast/stem cell growth factor receptor KitHomo sapiens (human)0.2639
Fibroblast growth factor receptor 1Homo sapiens (human)1.4228
AromataseHomo sapiens (human)0.018
Proto-oncogene tyrosine-protein kinase SrcHomo sapiens (human)0.2764
Platelet-derived growth factor receptor alphaHomo sapiens (human)0.061
Translocator proteinRattus norvegicus (Norway rat)0.039
Vascular endothelial growth factor receptor 1 Homo sapiens (human)0.0457
AcetylcholinesteraseHomo sapiens (human)5.87
Platelet-derived growth factor receptor alpha Mus musculus (house mouse)0.0186
Tyrosine-protein kinase receptor UFOHomo sapiens (human)0.009
G protein-coupled receptor kinase 5Homo sapiens (human)0.83
Vascular endothelial growth factor receptor 3Homo sapiens (human)0.0089
Vascular endothelial growth factor receptor 2Homo sapiens (human)0.1116
Receptor-type tyrosine-protein kinase FLT3Homo sapiens (human)0.0581
Casein kinase I isoform alphaHomo sapiens (human)0.001
Ribosomal protein S6 kinase alpha-3Homo sapiens (human)0.1839
5'-AMP-activated protein kinase catalytic subunit alpha-2Homo sapiens (human)0.0617
Mu-type opioid receptorCavia porcellus (domestic guinea pig)0.018
Angiopoietin-1 receptorHomo sapiens (human)0.018
Focal adhesion kinase 1Homo sapiens (human)1.6
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)3.8389
5'-AMP-activated protein kinase catalytic subunit alpha-1Homo sapiens (human)0.158
Ribosomal protein S6 kinase alpha-1Homo sapiens (human)0.1313
AP2-associated protein kinase 1Homo sapiens (human)0.0462
Leucine-rich repeat serine/threonine-protein kinase 2Homo sapiens (human)0.0215
Aurora kinase BHomo sapiens (human)1.5
Serine/threonine-protein kinase TBK1Homo sapiens (human)0.22
ALK tyrosine kinase receptorHomo sapiens (human)1.1773
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)3

Research

Studies (36)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's4 (11.11)29.6817
2010's27 (75.00)24.3611
2020's5 (13.89)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
Bullock, AN; Fedorov, O; Knapp, S; Marsden, B; Müller, S; Pogacic, V; Rellos, P; Schwaller, J; Sundström, M1
Archibald, H; Dowell, L; Drew, L; Erlander, MG; Gray, NS; Greninger, P; Haber, DA; Hanke, JH; Iafrate, AJ; Lamb, J; Lee, D; Ma, XJ; Maheswaran, S; McDermott, U; Montagut, C; Njauw, CN; Raudales, R; Rothenberg, SM; Settleman, J; Sharma, SV; Sordella, R; Supko, JG; Tam, A; Tsao, H; Ulkus, LE1
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
Morphy, R1
Gangjee, A; Ihnat, MA; Kurup, S; Shenoy, SS; Thorpe, JE1
Disch, BC; Gangjee, A; Ihnat, MA; Raghavan, S; Zhao, Y1
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
Disch, B; Gangjee, A; Ihnat, MA; Kurup, S; Thorpe, JE1
Bailey-Downs, LC; Gangjee, A; Ihnat, MA; Kisliuk, RL; Thorpe, JE; Zhao, Y1
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
Bailey-Downs, LC; Gangjee, A; Ihnat, MA; Namjoshi, OA; Thorpe, JE; Yu, J1
Bastian, A; Disch, BC; Gangjee, A; Ihnat, MA; Raghavan, S; Thorpe, JE; Zaware, N1
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
Balke-Want, H; Basu, D; Engel, J; Ercanoglu, MS; Rauh, D; Richters, A; Tesch, R; Thomas, RK1
Bastian, A; Gangjee, A; Hamel, E; Ihnat, M; Mooberry, SL; Raghavan, S; Zammiello, C; Zhang, X1
Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K1
Bestgen, B; Borjini, N; Chevé, G; Daydé-Cazals, B; Fauvel, B; Feneyrolles, C; Gassiot, F; Singer, M; Spenlinhauer, A; Van Hijfte, N; Warnault, P; Yasri, A1
Bai, R; Bastian, A; Choudhary, S; Gangjee, A; Hamel, E; Ihnat, MA; Pavana, RK1
Chen, EC; Chien, HC; Giacomini, KM; Huang, Y; Khuri, N; Liang, X; Sali, A; Stecula, A; Yee, SW1
Cai, W; Chen, QY; Dang, LH; Luesch, H1
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
Choudhary, S; Devambatla, RKV; Gangjee, A; Hamel, E; Ihnat, M; Mooberry, SL1
Baraldi, PG; Baraldi, S; Bortolozzi, R; Brancale, A; Chayah, M; Ferla, S; Hamel, E; Kimatrai Salvador, M; Lopez-Cara, LC; Mariotto, E; Mattiuzzo, E; Oliva, P; Prencipe, F; Romagnoli, R; Ronca, R; Schiaffino Ortega, S; Viola, G1
Abou-Zeid, LA; El-Mesery, M; El-Sayed, MA; Gomaa, RM; Mostafa, AS; Selim, KB; Zeidan, MA1
Chellappan, DK; Collet, TA; Dighe, SN; Dua, K; Ekwudu, O; Katavic, PL1
Asquith, CRM; Einav, S; Pu, SY; Saul, S; Zuercher, WJ1
Bharate, SB; Raghuvanshi, R1
Choudhary, S; Doshi, A; Gangjee, A; Hamel, E; Ihnat, M; Luckett-Chastain, L; Mooberry, SL1
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

Reviews

5 review(s) available for erlotinib and su 11248

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
Recent update on anti-dengue drug discovery.
    European journal of medicinal chemistry, 2019, Aug-15, Volume: 176

    Topics: Animals; Antiviral Agents; Biological Products; Cell Line, Tumor; Dengue Virus; Drug Discovery; Humans; Serine Proteinase Inhibitors; Viral Nonstructural Proteins; Virus Replication

2019
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

31 other study(ies) available for erlotinib and su 11248

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
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
Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling.
    Proceedings of the National Academy of Sciences of the United States of America, 2007, Dec-11, Volume: 104, Issue:50

    Topics: Antineoplastic Agents; Cell Line, Tumor; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Gene Expression Regulation, Neoplastic; Genotype; Humans; Neoplasms; Protein Kinase Inhibitors

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
Synthesis and biological activity of N(4)-phenylsubstituted-6-(2,4-dichloro phenylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic and antitumor agents.
    Bioorganic & medicinal chemistry, 2010, May-15, Volume: 18, Issue:10

    Topics: Angiogenesis Inhibitors; Animals; Antineoplastic Agents; Cell Line, Tumor; Diamines; Indoles; Male; Melanoma; Mice; Mice, Nude; Molecular Structure; Phosphorylation; Pyrimidines; Pyrimidinones; Pyrroles; Structure-Activity Relationship; Vascular Endothelial Growth Factor Receptor-2

2010
Design, synthesis and evaluation of 2-amino-4-m-bromoanilino-6-arylmethyl-7H-pyrrolo[2,3-d]pyrimidines as tyrosine kinase inhibitors and antiangiogenic agents.
    Bioorganic & medicinal chemistry, 2010, Jul-15, Volume: 18, Issue:14

    Topics: Angiogenesis Inhibitors; Cell Line, Tumor; ErbB Receptors; Humans; Models, Molecular; Protein Kinase Inhibitors; Pyrimidines; Receptor Protein-Tyrosine Kinases; Receptor, Platelet-Derived Growth Factor beta; Vascular Endothelial Growth Factor Receptor-2

2010
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
N⁴-Aryl-6-substitutedphenylmethyl-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines as receptor tyrosine kinase inhibitors.
    Bioorganic & medicinal chemistry, 2012, Jan-15, Volume: 20, Issue:2

    Topics: Antineoplastic Agents; Cell Line, Tumor; Diamines; Enzyme Activation; ErbB Receptors; Humans; Protein Kinase Inhibitors; Pyrimidines; Vascular Endothelial Growth Factor Receptor-1; Vascular Endothelial Growth Factor Receptor-2

2012
Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.
    Bioorganic & medicinal chemistry, 2012, Jul-15, Volume: 20, Issue:14

    Topics: Angiogenesis Inhibitors; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Chick Embryo; Drug Screening Assays, Antitumor; Humans; Indenes; Melanoma, Experimental; Mice; Pyrimidines; Receptor, Platelet-Derived Growth Factor beta

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
N2-Trimethylacetyl substituted and unsubstituted-N4-phenylsubstituted-6-(2-pyridin-2-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2,4-diamines: design, cellular receptor tyrosine kinase inhibitory activities and in vivo evaluation as antiangiogenic, antimetastati
    Bioorganic & medicinal chemistry, 2013, Mar-01, Volume: 21, Issue:5

    Topics: Angiogenesis Inhibitors; Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Survival; Disease Models, Animal; Drug Design; Humans; Melanoma, Experimental; Mice; Mice, Nude; Microwaves; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Receptor Protein-Tyrosine Kinases; Structure-Activity Relationship

2013
Synthesis and biological activity of 5-chloro-N⁴-substituted phenyl-9H-pyrimido[4,5-b]indole-2,4-diamines as vascular endothelial growth factor receptor-2 inhibitors and antiangiogenic agents.
    Bioorganic & medicinal chemistry, 2013, Apr-01, Volume: 21, Issue:7

    Topics: Angiogenesis Inhibitors; Cell Line, Tumor; Diamines; Halogenation; Humans; Indoles; Pyrimidines; Vascular Endothelial Growth Factor Receptor-2

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
Identification and further development of potent TBK1 inhibitors.
    ACS chemical biology, 2015, Jan-16, Volume: 10, Issue:1

    Topics: Animals; Cell Line; Drug Design; Humans; Macrophages; Mice; Molecular Docking Simulation; Molecular Structure; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Small Molecule Libraries; Structure-Activity Relationship

2015
The design, synthesis and biological evaluation of conformationally restricted 4-substituted-2,6-dimethylfuro[2,3-d]pyrimidines as multi-targeted receptor tyrosine kinase and microtubule inhibitors as potential antitumor agents.
    Bioorganic & medicinal chemistry, 2015, May-15, Volume: 23, Issue:10

    Topics: Angiogenesis Inhibitors; Animals; Cell Line, Tumor; Cell Proliferation; Chick Embryo; Drug Design; ErbB Receptors; Furans; Humans; Inhibitory Concentration 50; Microtubules; Molecular Docking Simulation; Molecular Dynamics Simulation; Neovascularization, Physiologic; Protein Kinase Inhibitors; Pyrimidines; Receptor, Platelet-Derived Growth Factor beta; Structure-Activity Relationship; Tubulin Modulators; Vascular Endothelial Growth Factor Receptor-2

2015
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.
    Journal of medicinal chemistry, 2016, 04-28, Volume: 59, Issue:8

    Topics: Animals; Cell Proliferation; Drug Design; Human Umbilical Vein Endothelial Cells; Humans; Indoles; Male; Mice; Patch-Clamp Techniques; Protein Kinase Inhibitors

2016
Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.
    Bioorganic & medicinal chemistry, 2017, 01-15, Volume: 25, Issue:2

    Topics: Angiogenesis Inhibitors; Antineoplastic Agents; Cell Line; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Humans; Microtubules; Molecular Docking Simulation; Molecular Structure; Neovascularization, Pathologic; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Receptor Protein-Tyrosine Kinases; Structure-Activity Relationship

2017
Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).
    Journal of medicinal chemistry, 2017, 04-13, Volume: 60, Issue:7

    Topics: Drug Discovery; HEK293 Cells; Humans; Ligands; Molecular Docking Simulation; Organic Cation Transporter 1; Small Molecule Libraries

2017
Apratoxin S10, a Dual Inhibitor of Angiogenesis and Cancer Cell Growth To Treat Highly Vascularized Tumors.
    ACS medicinal chemistry letters, 2017, Oct-12, Volume: 8, Issue:10

    Topics:

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
Design, synthesis and preclinical evaluation of 5-methyl-N
    Bioorganic & medicinal chemistry letters, 2018, 10-01, Volume: 28, Issue:18

    Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Mice; Molecular Docking Simulation; Molecular Structure; Neoplasms, Experimental; Protein Kinase Inhibitors; Pyrimidines; Receptor, Platelet-Derived Growth Factor beta; Structure-Activity Relationship; Vascular Endothelial Growth Factor Receptor-2

2018
Design, Synthesis, and Biological Evaluation of 6-Substituted Thieno[3,2- d]pyrimidine Analogues as Dual Epidermal Growth Factor Receptor Kinase and Microtubule Inhibitors.
    Journal of medicinal chemistry, 2019, 02-14, Volume: 62, Issue:3

    Topics: Apoptosis; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Colchicine; Drug Design; Drug Evaluation, Preclinical; Enzyme Activation; ErbB Receptors; HeLa Cells; Humans; Membrane Potential, Mitochondrial; Microtubules; Poly(ADP-ribose) Polymerases; Polymerization; Pyrimidines; Reactive Oxygen Species; Tubulin; Vascular Endothelial Growth Factor Receptor-2

2019
Design, synthesis and docking study of novel picolinamide derivatives as anticancer agents and VEGFR-2 inhibitors.
    European journal of medicinal chemistry, 2019, Apr-15, Volume: 168

    Topics: Antineoplastic Agents; Cell Cycle; Cell Line, Tumor; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Design; Humans; Molecular Docking Simulation; Molecular Structure; Picolinic Acids; Protein Kinase Inhibitors; Structure-Activity Relationship; Vascular Endothelial Growth Factor Receptor-2

2019
Potent antiviral activity of novel multi-substituted 4-anilinoquin(az)olines.
    Bioorganic & medicinal chemistry letters, 2020, 08-15, Volume: 30, Issue:16

    Topics: Aniline Compounds; Antiviral Agents; Dengue Virus; Dose-Response Relationship, Drug; Microbial Sensitivity Tests; Molecular Structure; Quinazolines; Structure-Activity Relationship

2020
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
Potential of substituted quinazolines to interact with multiple targets in the treatment of cancer.
    Bioorganic & medicinal chemistry, 2021, 04-01, Volume: 35

    Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; ErbB Receptors; Humans; Molecular Structure; Protein Kinase Inhibitors; Quinazolines; Structure-Activity Relationship; Vascular Endothelial Growth Factor Receptor-2

2021