Tozasertib
| Title | Journal |
|---|---|
| The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents. | Journal of medicinal chemistry 20150108 |
| Direct and indirect targeting of MYC to treat acute myeloid leukemia. | Cancer chemotherapy and pharmacology 20150101 |
| Discovery, synthesis, and characterization of an orally bioavailable, brain penetrant inhibitor of mixed lineage kinase 3. | Journal of medicinal chemistry 20131024 |
| The discovery of PLK4 inhibitors: (E)-3-((1H-Indazol-6-yl)methylene)indolin-2-ones as novel antiproliferative agents. | Journal of medicinal chemistry 20130808 |
| Identification of potent Yes1 kinase inhibitors using a library screening approach. | Bioorganic & medicinal chemistry letters 20130801 |
| A broad activity screen in support of a chemogenomic map for kinase signalling research and drug discovery. | The Biochemical journal 20130415 |
| Development of o-chlorophenyl substituted pyrimidines as exceptionally potent aurora kinase inhibitors. | Journal of medicinal chemistry 20120913 |
| Co-treatment with vorinostat synergistically enhances activity of Aurora kinase inhibitor against human breast cancer cells. | Breast cancer research and treatment 20120901 |
| Activation of Aurora-A is essential for neuronal migration via modulation of microtubule organization. | The Journal of neuroscience : the official journal of the Society for Neuroscience 20120808 |
| Repression of cancer cell senescence by PKCι. | Oncogene 20120802 |
| Gadd45a transcriptional induction elicited by the Aurora kinase inhibitor MK-0457 in Bcr-Abl-expressing cells is driven by Oct-1 transcription factor. | Leukemia research 20120801 |
| Synthesis, biological evaluation, and molecular docking studies of N,1,3-triphenyl-1H-pyrazole-4-carboxamide derivatives as anticancer agents. | Bioorganic & medicinal chemistry letters 20120601 |
| Acute sensitization of colon cancer cells to inflammatory cytokines by prophase arrest. | Biochemical pharmacology 20120501 |
| In vitro drug metabolism by C-terminally truncated human flavin-containing monooxygenase 3. | Biochemical pharmacology 20120215 |
| Targeting aurora kinases: a novel approach to curb the growth & chemoresistance of androgen refractory prostate cancer. | Current cancer drug targets 20120201 |
| Selective aurora kinase inhibitors identified using a taxol-induced checkpoint sensitivity screen. | ACS chemical biology 20120120 |
| Histone H3 covalent modifications driving response of BCR-ABL1+ cells sensitive and resistant to imatinib to Aurora kinase inhibitor MK-0457. | British journal of haematology 20120101 |
| Vincristine potentiates the anti-proliferative effect of an aurora kinase inhibitor, VE-465, in myeloid leukemia cells. | Biochemical pharmacology 20111215 |
| Mutants of protein kinase A that mimic the ATP-binding site of Aurora kinase. | The Biochemical journal 20111115 |
| Comprehensive assay of kinase catalytic activity reveals features of kinase inhibitor selectivity. | Nature biotechnology 20111101 |
| Comprehensive analysis of kinase inhibitor selectivity. | Nature biotechnology 20111030 |
| An integrated chemical biology approach identifies specific vulnerability of Ewing's sarcoma to combined inhibition of Aurora kinases A and B. | Molecular cancer therapeutics 20111001 |
| Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors. | Bioorganic & medicinal chemistry letters 20110915 |
| A novel cell-based, high-content assay for phosphorylation of Lats2 by Aurora A. | Journal of biomolecular screening 20110901 |
| Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives. | European journal of medicinal chemistry 20110601 |
| Combining histone deacetylase inhibitor vorinostat with aurora kinase inhibitors enhances lymphoma cell killing with repression of c-Myc, hTERT, and microRNA levels. | Cancer research 20110601 |
| VX680 binding in Aurora A: π-π interactions involving the conserved aromatic amino acid of the flexible glycine-rich loop. | The journal of physical chemistry. A 20110428 |
| Crystal structures of ABL-related gene (ABL2) in complex with imatinib, tozasertib (VX-680), and a type I inhibitor of the triazole carbothioamide class. | Journal of medicinal chemistry 20110414 |
| Phthalazinone pyrazoles as potent, selective, and orally bioavailable inhibitors of Aurora-A kinase. | Journal of medicinal chemistry 20110113 |
| Inhibition of mitotic kinase Aurora suppresses Akt-1 activation and induces apoptotic cell death in all-trans retinoid acid-resistant acute promyelocytic leukemia cells. | Journal of translational medicine 20110101 |
| Inhibition of proliferation, viability, migration and invasion of gastric cancer cells by Aurora-A deletion. | Asian Pacific journal of cancer prevention : APJCP 20110101 |
| Preclinical evaluation of AMG 900, a novel potent and highly selective pan-aurora kinase inhibitor with activity in taxane-resistant tumor cell lines. | Cancer research 20101201 |
| Activation state-dependent binding of small molecule kinase inhibitors: structural insights from biochemistry. | Chemistry & biology 20101124 |
| Efficacy of MK-0457 and in combination with vorinostat against Philadelphia chromosome positive acute lymphoblastic leukemia cells. | Annals of hematology 20101101 |
| Evaluation of an Actinomycin D/VX-680 aurora kinase inhibitor combination in p53-based cyclotherapy. | Oncotarget 20101101 |
| Combination of nutlin-3 and VX-680 selectively targets p53 mutant cells with reversible effects on cells expressing wild-type p53. | Cell death and differentiation 20100901 |
| A type-II kinase inhibitor capable of inhibiting the T315I 'gatekeeper' mutant of Bcr-Abl. | Journal of medicinal chemistry 20100812 |
| 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors. | Bioorganic & medicinal chemistry letters 20100801 |
| Fast-forwarding hit to lead: aurora and epidermal growth factor receptor kinase inhibitor lead identification. | Journal of medicinal chemistry 20100708 |
| Discovery of GSK1070916, a potent and selective inhibitor of Aurora B/C kinase. | Journal of medicinal chemistry 20100527 |
| Activity of the Aurora kinase inhibitor VX-680 against Bcr/Abl-positive acute lymphoblastic leukemias. | Molecular cancer therapeutics 20100501 |
| Targets and effectors of the cellular response to aurora kinase inhibitor MK-0457 (VX-680) in imatinib sensitive and resistant chronic myelogenous leukemia. | Biochemical pharmacology 20100301 |
| Inhibition of the aurora kinases suppresses in vitro NT2-D1 cell growth and tumorigenicity. | The Journal of endocrinology 20100201 |
| In vitro anti-myeloma activity of the Aurora kinase inhibitor VE-465. | British journal of haematology 20091201 |
| Overcoming resistance in chronic myelogenous leukemia. | Leukemia & lymphoma 20091101 |
| The Aurora Kinase in Trypanosoma brucei plays distinctive roles in metaphase-anaphase transition and cytokinetic initiation. | PLoS pathogens 20090901 |
| The discovery of the potent aurora inhibitor MK-0457 (VX-680). | Bioorganic & medicinal chemistry letters 20090701 |
| Discovery and exploitation of inhibitor-resistant aurora and polo kinase mutants for the analysis of mitotic networks. | The Journal of biological chemistry 20090605 |
| Multitargeted sequential therapy with MK-0457 and dasatinib followed by stem cell transplantation for T315I mutated chronic myeloid leukemia. | Leukemia research 20090601 |
| Discovery and development of aurora kinase inhibitors as anticancer agents. | Journal of medicinal chemistry 20090514 |
| Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time1. | The Biochemical journal 20090513 |
| Short and long-term tumor cell responses to Aurora kinase inhibitors. | Experimental cell research 20090415 |
| Identification of genes that confer tumor cell resistance to the aurora B kinase inhibitor, AZD1152. | The pharmacogenomics journal 20090401 |
| Mechanism of MK-0457 efficacy against BCR-ABL positive leukemia cells. | Biochemical and biophysical research communications 20090320 |
| [Recent advance in the study of novel anti-tumor targets and drugs--aurora kinase and Pin1]. | Yao xue xue bao = Acta pharmaceutica Sinica 20090301 |
| Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. | Journal of medicinal chemistry 20090122 |
| Aurora-A down-regulates IkappaBalpha via Akt activation and interacts with insulin-like growth factor-1 induced phosphatidylinositol 3-kinase pathway for cancer cell survival. | Molecular cancer 20090101 |
| Assessment of chemical coverage of kinome space and its implications for kinase drug discovery. | Journal of medicinal chemistry 20081225 |
| Aurora A is essential for early embryonic development and tumor suppression. | The Journal of biological chemistry 20081114 |
| Concomitant inhibition of Mdm2-p53 interaction and Aurora kinases activates the p53-dependent postmitotic checkpoints and synergistically induces p53-mediated mitochondrial apoptosis along with reduced endoreduplication in acute myelogenous leukemia. | Blood 20081001 |
| Modulation of kinase-inhibitor interactions by auxiliary protein binding: crystallography studies on Aurora A interactions with VX-680 and with TPX2. | Protein science : a publication of the Protein Society 20081001 |
| Inhibition of Aurora-A suppresses epithelial-mesenchymal transition and invasion by downregulating MAPK in nasopharyngeal carcinoma cells. | Carcinogenesis 20081001 |
| Cotreatment with vorinostat enhances activity of MK-0457 (VX-680) against acute and chronic myelogenous leukemia cells. | Clinical cancer research : an official journal of the American Association for Cancer Research 20081001 |
| Targeting aurora kinase with MK-0457 inhibits ovarian cancer growth. | Clinical cancer research : an official journal of the American Association for Cancer Research 20080901 |
| Vorinostat synergistically potentiates MK-0457 lethality in chronic myelogenous leukemia cells sensitive and resistant to imatinib mesylate. | Blood 20080801 |
| [Novel medical treatment modalities in hematology]. | Ugeskrift for laeger 20080609 |
| Activity of a novel Aurora kinase inhibitor against the T315I mutant form of BCR-ABL: in vitro and in vivo studies. | Cancer science 20080601 |
| Effects of the Aurora kinase inhibitor VX-680 on anaplastic thyroid cancer-derived cell lines. | Endocrine-related cancer 20080601 |
| Aurora kinase inhibitory VX-680 increases Bax/Bcl-2 ratio and induces apoptosis in Aurora-A-high acute myeloid leukemia. | Blood 20080301 |
| Aurora kinase A inhibitors: identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold. | Bioorganic & medicinal chemistry letters 20080301 |
| Spatio-temporal expression patterns of aurora kinases a, B, and C and cytoplasmic polyadenylation-element-binding protein in bovine oocytes during meiotic maturation. | Biology of reproduction 20080201 |
| A quantitative analysis of kinase inhibitor selectivity. | Nature biotechnology 20080101 |
| Inhibitors of ABL and the ABL-T315I mutation. | Current topics in medicinal chemistry 20080101 |
| Aurora kinase inhibitors synergize with paclitaxel to induce apoptosis in ovarian cancer cells. | Journal of translational medicine 20080101 |
| The selectivity of protein kinase inhibitors: a further update. | The Biochemical journal 20071215 |
| [Acute lymphoblastic leukemia with Philadelphia chromosome: treatment with kinase inhibitors]. | Bulletin du cancer 20071001 |
| Sequential ABL kinase inhibitor therapy selects for compound drug-resistant BCR-ABL mutations with altered oncogenic potency. | The Journal of clinical investigation 20070904 |
| Hepatic metabolism of MK-0457, a potent aurora kinase inhibitor: interspecies comparison and role of human cytochrome P450 and flavin-containing monooxygenase. | Drug metabolism and disposition: the biological fate of chemicals 20070901 |
| Transforming acidic coiled-coil 3 and Aurora-A interact in human thyrocytes and their expression is deregulated in thyroid cancer tissues. | Endocrine-related cancer 20070901 |
| Structural basis for potent inhibition of the Aurora kinases and a T315I multi-drug resistant mutant form of Abl kinase by VX-680. | Cancer letters 20070628 |
| [Novel anti-CML agents beyond imatinib]. | [Rinsho ketsueki] The Japanese journal of clinical hematology 20070601 |
| Targeted therapy and the T315I mutation in Philadelphia-positive leukemias. | Haematologica 20070401 |
| New blood cancer therapies under study. | JAMA 20070207 |
| With targeted drugs, chronic myelogenous leukemia therapy may follow HIV's model. | Journal of the National Cancer Institute 20070207 |
| MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation. | Blood 20070115 |
| Aurora kinase inhibition downregulates NF-kappaB and sensitises tumour cells to chemotherapeutic agents. | Biochemical and biophysical research communications 20070105 |
| Analysis of mitotic phosphorylation of borealin. | BMC cell biology 20070101 |
| Microsphere-based protease assays and screening application for lethal factor and factor Xa. | Cytometry. Part A : the journal of the International Society for Analytical Cytology 20060501 |
| Discovery of novel and potent thiazoloquinazolines as selective Aurora A and B kinase inhibitors. | Journal of medicinal chemistry 20060209 |
| Structure of the kinase domain of an imatinib-resistant Abl mutant in complex with the Aurora kinase inhibitor VX-680. | Cancer research 20060115 |
| Anticancer Drug Discovery and Development - SRI's Seventh Annual Summit. | IDrugs : the investigational drugs journal 20051001 |
| Dawn of Aurora kinase inhibitors as anticancer drugs. | Expert opinion on investigational drugs 20040901 |
| VX-680, a potent and selective small-molecule inhibitor of the Aurora kinases, suppresses tumor growth in vivo. | Nature medicine 20040301 |