Aurora kinase inhibitors: Progress towards the clinic

Phase 1/2 study to assess the safety, efficacy, and pharmacokinetics of barasertib (AZD1152) in patients with advanced acute myeloid leukemia

(2011) B. Lowenberg et al.   BLOOD

Phase I, open-label, multicentre, dose-escalation, pharmacokinetic and pharmacodynamic trial of the oral aurora kinase inhibitor PF-03814735 in advanced solid tumours

(2011) Patrick Schöffski et al.   EUROPEAN JOURNAL OF CANCER

Clinical evaluation of AZD1152, an i.v. inhibitor of Aurora B kinase, in patients with solid malignant tumors

(2010) D. S. Boss et al.   ANNALS OF ONCOLOGY

Activity of the multitargeted kinase inhibitor, AT9283, in imatinib-resistant BCR-ABL-positive leukemic cells

(2010) R. Tanaka et al.   BLOOD

A novel Aurora-A kinase inhibitor MLN8237 induces cytotoxicity and cell-cycle arrest in multiple myeloma

(2010) G. Gorgun et al.   BLOOD

Preclinical activity of a novel multiple tyrosine kinase and aurora kinase inhibitor, ENMD-2076, against multiple myeloma

(2010) Xiaojing Wang et al.   BRITISH JOURNAL OF HAEMATOLOGY

Preclinical Evaluation of AMG 900, a Novel Potent and Highly Selective Pan-Aurora Kinase Inhibitor with Activity in Taxane-Resistant Tumor Cell Lines

(2010) M. Payton et al.   CANCER RESEARCH

Phase I Safety, Pharmacokinetic, and Pharmacodynamic Study of ENMD-2076, a Novel Angiogenic and Aurora Kinase Inhibitor,in Patients with Advanced Solid Tumors

(2010) J. R. Diamond et al.   CLINICAL CANCER RESEARCH

Assessment of the In vivo Antitumor Effects of ENMD-2076, a Novel Multitargeted Kinase Inhibitor, against Primary and Cell Line-Derived Human Colorectal Cancer Xenograft Models

(2010) J. J. Tentler et al.   CLINICAL CANCER RESEARCH

The novel Aurora A kinase inhibitor MLN8237 is active in resistant chronic myeloid leukaemia and significantly increases the efficacy of nilotinib

(2010) Kevin R. Kelly et al.   JOURNAL OF CELLULAR AND MOLECULAR MEDICINE

Discovery ofN-Phenyl-4-(thiazol-5-yl)pyrimidin-2-amine Aurora Kinase Inhibitors

(2010) Shudong Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of GSK1070916, a Potent and Selective Inhibitor of Aurora B/C Kinase

(2010) Nicholas D. Adams et al.   JOURNAL OF MEDICINAL CHEMISTRY

ENMD-2076 Is an Orally Active Kinase Inhibitor with Antiangiogenic and Antiproliferative Mechanisms of Action

(2010) G. C. Fletcher et al.   MOLECULAR CANCER THERAPEUTICS

PF-03814735, an Orally Bioavailable Small Molecule Aurora Kinase Inhibitor for Cancer Therapy

(2010) Jitesh P. Jani et al.   MOLECULAR CANCER THERAPEUTICS

MK-5108, a Highly Selective Aurora-A Kinase Inhibitor, Shows Antitumor Activity Alone and in Combination with Docetaxel

(2010) T. Shimomura et al.   MOLECULAR CANCER THERAPEUTICS

Biochemical characterization of GSK1070916, a potent and selective inhibitor of Aurora B and Aurora C kinases with an extremely long residence time1

(2009) Kelly Anderson et al.   BIOCHEMICAL JOURNAL

The discovery of the potent aurora inhibitor MK-0457 (VX-680)

(2009) David Bebbington et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

In vitroanti-myeloma activity of the Aurora kinase inhibitor VE-465

(2009) Joseph M. Negri et al.   BRITISH JOURNAL OF HAEMATOLOGY

SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo

(2009) Jennifer P. Arbitrario et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

A Phase I Dose-Escalation Study of Danusertib (PHA-739358) Administered as a 24-Hour Infusion with and without Granulocyte Colony-Stimulating Factor in a 14-Day Cycle in Patients with Advanced Solid Tumors

(2009) R. B. Cohen et al.   CLINICAL CANCER RESEARCH

Preclinical characterization of Aurora kinase inhibitor R763/AS703569 identified through an image-based phenotypic screen

(2009) John McLaughlin et al.   JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY

A Class of 2,4-Bisanilinopyrimidine Aurora A Inhibitors with Unusually High Selectivity against Aurora B†

(2009) Ignacio Aliagas-Martin et al.   JOURNAL OF MEDICINAL CHEMISTRY

GSK1070916, a potent Aurora B/C kinase inhibitor with broad antitumor activity in tissue culture cells and human tumor xenograft models

(2009) M. A. Hardwicke et al.   MOLECULAR CANCER THERAPEUTICS

Identification of genes that confer tumor cell resistance to the Aurora B kinase inhibitor, AZD1152

(2009) J Guo et al.   PHARMACOGENOMICS JOURNAL

Discovery of an Aurora kinase inhibitor through site-specific dynamic combinatorial chemistry

(2008) Mark T. Cancilla et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Discovery of a potent and selective Aurora kinase inhibitor

(2008) Johan D. Oslob et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Molecular Basis of Drug Resistance in Aurora Kinases

(2008) Fiona Girdler et al.   CHEMISTRY & BIOLOGY

280 POSTER Phase I study of the safety, pharmacokinetics (PK), and pharmacodynamics (PD) of MLN8237, a selective Aurora A kinase inhibitor, in the United States

(2008) J. Infante et al.   EJC SUPPLEMENTS

The Aurora kinase inhibitor VE-465 has anticancer effects in pre-clinical studies of human hepatocellular carcinoma

(2008) Zhong-Zhe Lin et al.   JOURNAL OF HEPATOLOGY

A Pentacyclic Aurora Kinase Inhibitor (AKI-001) with High in Vivo Potency and Oral Bioavailability∞

(2008) Thomas E. Rawson et al.   JOURNAL OF MEDICINAL CHEMISTRY

Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity†

(2008) Steven Howard et al.   JOURNAL OF MEDICINAL CHEMISTRY

Elevated expressions of survivin and VEGF protein are strong independent predictors of survival in advanced nasopharyngeal carcinoma

(2008) Yu-Hong Li et al.   Journal of Translational Medicine

Jadomycin B, an Aurora-B kinase inhibitor discovered through virtual screening

(2008) D.-H. Fu et al.   MOLECULAR CANCER THERAPEUTICS

Modulation of kinase-inhibitor interactions by auxiliary protein binding: Crystallography studies on Aurora A interactions with VX-680 and with TPX2

(2008) Baoguang Zhao et al.   PROTEIN SCIENCE