Kinesin spindle protein inhibitors in cancer: a patent review (2008 – present)

Progress on Kinesin Spindle Protein Inhibitors as Anti-Cancer Agents

(2013) Yingjie Zhang et al.   Anti-Cancer Agents in Medicinal Chemistry

Advances in the discovery of kinesin spindle protein (Eg5) inhibitors as antitumor agents

(2013) Hala Bakr El-Nassan   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Doing the methylene shuffle – Further insights into the inhibition of mitotic kinesin Eg5 with S-trityl l-cysteine

(2012) Murad N. Abualhasan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Triphenylbutanamines: Kinesin Spindle Protein Inhibitors with in Vivo Antitumor Activity

(2012) Fang Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Receptor–Ligand Interaction-Based Virtual Screening for Novel Eg5/Kinesin Spindle Protein Inhibitors

(2012) Shanthi Nagarajan et al.   JOURNAL OF MEDICINAL CHEMISTRY

A potent chemotherapeutic strategy in prostate cancer: S-(methoxytrityl)-L-cysteine, a novel Eg5 inhibitor

(2011) Nai-Dong Xing et al.   ASIAN JOURNAL OF ANDROLOGY

Synthesis and characterization of tritylthioethanamine derivatives with potent KSP inhibitory activity

(2011) Delany Rodriguez et al.   BIOORGANIC & MEDICINAL CHEMISTRY

De novo design, synthesis and biological evaluation of 1,4-dihydroquinolin-4-ones and 1,2,3,4-tetrahydroquinazolin-4-ones as potent kinesin spindle protein (KSP) inhibitors

(2011) Cheng Jiang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A phase 1 dose-escalation study of ARRY-520, a kinesin spindle protein inhibitor, in patients with advanced myeloid leukemias

(2011) Hanna Jean Khoury et al.   CANCER

A phase I trial of MK-0731, a Kinesin Spindle Protein (KSP) inhibitor, in patients with solid tumors

(2011) Kyle Holen et al.   INVESTIGATIONAL NEW DRUGS

Structure–Activity Relationships of Carboline and Carbazole Derivatives as a Novel Class of ATP-Competitive Kinesin Spindle Protein Inhibitors

(2011) Tomoki Takeuchi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure−Activity Relationship and Multidrug Resistance Study of NewS-trityl-l-Cysteine Derivatives As Inhibitors of Eg5

(2011) Hung Yi Kristal Kaan et al.   JOURNAL OF MEDICINAL CHEMISTRY

CPUYJ039, a newly synthesized benzimidazole-based compound, is proved to be a novel inducer of apoptosis in HCT116 cells with potent KSP inhibitory activity

(2011) Cheng Jiang et al.   JOURNAL OF PHARMACY AND PHARMACOLOGY

Discovery of tetrahydro-β-carbolines as inhibitors of the mitotic kinesin KSP

(2010) Fei Liu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and bioevaluation of dihydropyrazolo[3,4-b]pyridine and benzo[4,5]imidazo[1,2-a]pyrimidine compounds as dual KSP and Aurora-A kinase inhibitors for anti-cancer agents

(2010) Rong-geng Fu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Monastrol analogs: A synthesis of pyrazolopyridine, benzopyranopyrazolopyridine, and oxygen-bridged azolopyrimidine derivatives and their biological screening

(2010) Jan Svetlik et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Biochemical analysis of cellular target of S-trityl-l-cysteine derivatives using affinity matrix

(2010) Makiko Shimizu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A first in human study of SB-743921, a kinesin spindle protein inhibitor, to determine pharmacokinetics, biologic effects and establish a recommended phase II dose

(2010) Kyle D. Holen et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

S-trityl-L-cysteine derivative induces caspase-independent cell death in K562 human chronic myeloid leukemia cell line

(2010) Makiko Shimizu et al.   CANCER LETTERS

Structure-Activity Relationships and Molecular Docking of Novel Dihydropyrimidine-Based Mitotic Eg5 Inhibitors

(2010) Hana Prokopcová et al.   ChemMedChem

Activity of the Kinesin Spindle Protein Inhibitor Ispinesib (SB-715992) in Models of Breast Cancer

(2010) J. W. Purcell et al.   CLINICAL CANCER RESEARCH

Kinesin Spindle Protein (KSP) Inhibitors with 2,3-Fused Indole Scaffolds

(2010) Shinya Oishi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structural Basis for Inhibition of Eg5 by Dihydropyrimidines: Stereoselectivity of Antimitotic Inhibitors Enastron, Dimethylenastron and Fluorastrol

(2010) Hung Yi Kristal Kaan et al.   JOURNAL OF MEDICINAL CHEMISTRY

A Potent Chemotherapeutic Strategy for Bladder Cancer: (S)-Methoxy-Trityl-L-Cystein, a Novel Eg5 Inhibitor

(2010) Sentai Ding et al.   JOURNAL OF UROLOGY

SCH 2047069, a Novel Oral Kinesin Spindle Protein Inhibitor, Shows Single-Agent Antitumor Activity and Enhances the Efficacy of Chemotherapeutics

(2010) A. D. Basso et al.   MOLECULAR CANCER THERAPEUTICS

A pediatric phase I trial and pharmacokinetic study of ispinesib: A Children's Oncology Group phase I consortium study

(2010) Abdul-Kader Souid et al.   PEDIATRIC BLOOD & CANCER

The first highly stereoselective approach to the mitotic kinesin Eg5 inhibitor HR22C16 and its analogues

(2010) Sen Xiao et al.   TETRAHEDRON-ASYMMETRY

An allosteric transition trapped in an intermediate state of a new kinesin–inhibitor complex

(2009) Hung Yi Kristal Kaan et al.   BIOCHEMICAL JOURNAL

Bis(hetero)aryl derivatives as unique kinesin spindle protein inhibitors

(2009) Kenji Matsuno et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Substituted benzimidazoles: A novel chemotype for small molecule hKSP inhibitors

(2009) Brian R. Lahue et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

The discovery of tetrahydro-β-carbolines as inhibitors of the kinesin Eg5

(2009) Paul A. Barsanti et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

K858, a Novel Inhibitor of Mitotic Kinesin Eg5 and Antitumor Agent, Induces Cell Death in Cancer Cells

(2009) R. Nakai et al.   CANCER RESEARCH

Design, Synthesis and Evaluation of Tetrahydroisoquinolines as New Kinesin Spindle Protein Inhibitors

(2009) Cheng Jiang et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

KSP inhibitor ARRY-520 as a substitute for Paclitaxel in Type I ovarian cancer cells

(2009) Ki Hyung Kim et al.   Journal of Translational Medicine

Inhibition of KSP by ARRY-520 induces cell cycle block and cell death via the mitochondrial pathway in AML cells

(2009) B Z Carter et al.   LEUKEMIA

Initial testing (stage 1) of the kinesin spindle protein inhibitor ispinesib by the pediatric preclinical testing program

(2009) Hernan Carol et al.   PEDIATRIC BLOOD & CANCER

Crystal structure of HsEg5 in complex with clinical candidate CK0238273 provides insight into inhibitory mechanism, potency, and specificity

(2008) Bin Zhang et al.   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Validating the mitotic kinesin Eg5 as a therapeutic target in pancreatic cancer cells and tumor xenografts using a specific inhibitor

(2008) Min Liu et al.   BIOCHEMICAL PHARMACOLOGY

Cloning, Enzyme Characterization of Recombinant Human Eg5 and the Development of a New Inhibitor

(2008) Lei Yang et al.   BIOLOGICAL & PHARMACEUTICAL BULLETIN

Southwest Oncology Group Phase II Study of Ispinesib in Androgen-Independent Prostate Cancer Previously Treated with Taxanes

(2008) Tomasz M. Beer et al.   Clinical Genitourinary Cancer

Recent Progress in the Identification and Clinical Evaluation of Inhibitors of the Mitotic Kinesin KSP

(2008) Steven Knight et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Therapeutic potential of mitotic kinesin inhibitors in cancer

(2008) Kenji Matsuno et al.   EXPERT OPINION ON THERAPEUTIC PATENTS

Kinesin Spindle Protein (KSP) Inhibitors. 9. Discovery of (2S)-4-(2,5-Difluorophenyl)-N-[(3R,4S)-3-fluoro-1-methylpiperidin-4-yl]-2-(hydroxymethyl)-N-methyl-2-phenyl-2,5-dihydro-1H-pyrrole-1-carboxamide (MK-0731) for the Treatment of Taxane-Refractory Cancer

(2008) Christopher D. Cox et al.   JOURNAL OF MEDICINAL CHEMISTRY

Structure–Activity Relationship ofS-Trityl-l-Cysteine Analogues as Inhibitors of the Human Mitotic Kinesin Eg5

(2008) Salvatore DeBonis et al.   JOURNAL OF MEDICINAL CHEMISTRY

Effects of Eg5 knockdown on human prostate cancer xenograft growth and chemosensitivity

(2008) Norihiro Hayashi et al.   PROSTATE