An Overview of Tubulin Inhibitors That Interact with the Colchicine Binding Site

Synthesis and Biological Evaluation of 1,4-Diaryl-2-azetidinones as Specific Anticancer Agents: Activation of Adenosine Monophosphate Activated Protein Kinase and Induction of Apoptosis

(2012) Farida Tripodi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Substituted 3-(5-Imidazo[2,1-b]thiazolylmethylene)-2-indolinones and Analogues: Synthesis, Cytotoxic Activity, and Study of the Mechanism of Action

(2012) Aldo Andreani et al.   JOURNAL OF MEDICINAL CHEMISTRY

4,5-Diaryl-3-aminopyrazole Derivatives as Analogs of Combretastatin A-4: Synthesis and Biological Evaluation

(2011) Tao Liu et al.   ARCHIV DER PHARMAZIE

Acetyl analogs of combretastatin A-4: Synthesis and biological studies

(2011) Balaji Babu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Phenylimino-10H-anthracen-9-ones as novel antimicrotubule agents—synthesis, antiproliferative activity and inhibition of tubulin polymerization

(2011) Helge Prinz et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, biological evaluation, and molecular modeling of cinnamic acyl sulfonamide derivatives as novel antitubulin agents

(2011) Yin Luo et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Antitumor agents 283. Further elaboration of Desmosdumotin C analogs as potent antitumor agents: Activation of spindle assembly checkpoint as possible mode of action

(2011) Kyoko Nakagawa-Goto et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, biological evaluation, and molecular docking studies of resveratrol derivatives possessing chalcone moiety as potential antitubulin agents

(2011) Ban-Feng Ruan et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, biological evaluation and molecular modeling of 1,2,3-triazole analogs of combretastatin A-1

(2011) Øyvind W. Akselsen et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A phase I study of MN-029 (denibulin), a novel vascular-disrupting agent, in patients with advanced solid tumors

(2011) Alejandro D. Ricart et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

UA62784 Is a Cytotoxic Inhibitor of Microtubules, not CENP-E

(2011) Sergey Tcherniuk et al.   CHEMISTRY & BIOLOGY

Clinical, Pharmacodynamic, and Pharmacokinetic Evaluation of BNC105P: A Phase I Trial of a Novel Vascular Disrupting Agent and Inhibitor of Cancer Cell Proliferation

(2011) D. Rischin et al.   CLINICAL CANCER RESEARCH

A novel class of trans-methylpyrazoline analogs of combretastatins: Synthesis and in-vitro biological testing

(2011) Megan Lee et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of 1-(4′-Indolyl and 6′-Quinolinyl) indoles as a new class of potent anticancer agents

(2011) Mei-Jung Lai et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Substituted phenyl 4-(2-oxoimidazolidin-1-yl)benzenesulfonamides as antimitotics. Antiproliferative, antiangiogenic and antitumoral activity, and quantitative structure-activity relationships

(2011) Sébastien Fortin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, molecular docking study and antitumor activity of novel 2-phenylindole derivatives

(2011) Sally S. El-Nakkady et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Liposomes as carriers for colchicine-derived prodrugs: Vascular disrupting nanomedicines with tailorable drug release kinetics

(2011) Bart J. Crielaard et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

A polymeric colchicinoid prodrug with reduced toxicity and improved efficacy for vascular disruption in cancer therapy

(2011) Bart J. Crielaard et al.   International Journal of Nanomedicine

Molecular cytogenetic evaluation of the mechanism of genotoxic potential of amsacrine and nocodazole in mouse bone marrow cells

(2011) Sabry M. Attia   JOURNAL OF APPLIED TOXICOLOGY

Rational design, synthesis and biological evaluations of amino-noscapine: a high affinity tubulin-binding noscapinoid

(2011) Pradeep K. Naik et al.   JOURNAL OF COMPUTER-AIDED MOLECULAR DESIGN

Synthesis and Biological Evaluation of 2,4,5-Substituted Pyrimidines as a New Class of Tubulin Polymerization Inhibitors

(2011) Fuchun Xie et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Biological Activities of (R)- and (S)-N-(4-Methoxyphenyl)-N,2,6-trimethyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-aminium Chloride as Potent Cytotoxic Antitubulin Agents

(2011) Aleem Gangjee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antitumor Agents. 284. New Desmosdumotin B Analogues with Bicyclic B-Ring as Cytotoxic and Antitubulin Agents

(2011) Kyoko Nakagawa-Goto et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Biological Evaluation of 4-Arylcoumarin Analogues of Combretastatins. Part 2

(2011) Sébastien Combes et al.   JOURNAL OF MEDICINAL CHEMISTRY

Convergent Synthesis and Biological Evaluation of 2-Amino-4-(3′,4′,5′-trimethoxyphenyl)-5-aryl Thiazoles as Microtubule Targeting Agents

(2011) Romeo Romagnoli et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and Synthesis of 2-Heterocyclyl-3-arylthio-1H-indoles as Potent Tubulin Polymerization and Cell Growth Inhibitors with Improved Metabolic Stability

(2011) Giuseppe La Regina et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, Biological Evaluation, and Structure–Activity Relationships of Substituted Phenyl 4-(2-Oxoimidazolidin-1-yl)benzenesulfonates as New Tubulin Inhibitors Mimicking Combretastatin A-4

(2011) Sébastien Fortin et al.   JOURNAL OF MEDICINAL CHEMISTRY

Regioselective Suzuki Coupling of Dihaloheteroaromatic Compounds as a Rapid Strategy To Synthesize Potent Rigid Combretastatin Analogues

(2011) Sewan Theeramunkong et al.   JOURNAL OF MEDICINAL CHEMISTRY

5-Amino-2-aroylquinolines as Highly Potent Tubulin Polymerization Inhibitors. Part 2. The Impact of Bridging Groups at Position C-2

(2011) Hsueh-Yun Lee et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Structure–Activity Relationship Study of Antimicrotubule Agents Phenylahistin Derivatives with a Didehydropiperazine-2,5-dione Structure

(2011) Yuri Yamazaki et al.   JOURNAL OF MEDICINAL CHEMISTRY

Rigid Analogues of Antimitotic Indolobenzazepinones: New Insights into Tubulin Binding via Molecular Modeling

(2011) Valérie Pons et al.   ACS Medicinal Chemistry Letters

A Phase Ib trial of CA4P (combretastatin A-4 phosphate), carboplatin and paclitaxel in patients with advanced cancer

(2010) G J Rustin et al.   BRITISH JOURNAL OF CANCER

Biological Activity of 4-Substituted Methoxybenzoyl- Aryl-Thiazole: An Active Microtubule Inhibitor

(2010) C.-M. Li et al.   CANCER RESEARCH

BPR0C261 is a novel orally active antitumor agent with antimitotic and anti-angiogenic activities

(2010) Chih-Bo Hu et al.   CANCER SCIENCE

Domino approach to 2-aroyltrimethoxyindoles as novel heterocyclic combretastatin A4 analogues

(2010) Martin Arthuis et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

MT119, a new planar-structured compound, targets the colchicine site of tubulin arresting mitosis and inhibiting tumor cell proliferation

(2010) Zhixiang Zhang et al.   INTERNATIONAL JOURNAL OF CANCER

Stathmin and Interfacial Microtubule Inhibitors Recognize a Naturally Curved Conformation of Tubulin Dimers

(2010) Pascale Barbier et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synthesis, formulation and in vitro evaluation of a novel microtubule destabilizer, SMART-100

(2010) Feng Li et al.   JOURNAL OF CONTROLLED RELEASE

Synthesis, Antitubulin, and Antiproliferative SAR of Analogues of 2-Methoxyestradiol-3,17-O,O-bis-sulfamate

(2010) Fabrice Jourdan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of Novel 2-Aryl-4-benzoyl-imidazoles Targeting the Colchicines Binding Site in Tubulin As Potential Anticancer Agents

(2010) Jianjun Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

4-(3-Halo/amino-4,5-dimethoxyphenyl)-5-aryloxazoles and -N-methylimidazoles That Are Cytotoxic against Combretastatin A Resistant Tumor Cells and Vascular Disrupting in a Cisplatin Resistant Germ Cell Tumor Model

(2010) Rainer Schobert et al.   JOURNAL OF MEDICINAL CHEMISTRY

5-Amino-2-Aroylquinolines as Highly Potent Tubulin Polymerization Inhibitors

(2010) Chih-Ying Nien et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Evaluation of Azetidinone Analogues of Combretastatin A-4 as Tubulin Targeting Agents

(2010) Niamh M. O’Boyle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Pharmacological Evaluation ofN-(3-(1H-Indol-4-yl)-5-(2-methoxyisonicotinoyl)phenyl)methanesulfonamide (LP-261), a Potent Antimitotic Agent

(2010) Rupa S. Shetty et al.   JOURNAL OF MEDICINAL CHEMISTRY

ELR510444, A Novel Microtubule Disruptor with Multiple Mechanisms of Action

(2010) A. L. Risinger et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Characterization of the Covalent Binding of N-Phenyl-N'-(2-chloroethyl)ureas to  -Tubulin: Importance of Glu198 in Microtubule Stability

(2010) S. Fortin et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

ENMD-1198, a New Analogue of 2-Methoxyestradiol, Displays Both Antiangiogenic and Vascular-Disrupting Properties

(2010) E. Pasquier et al.   MOLECULAR CANCER THERAPEUTICS

Phase I Clinical Trial of MPC-6827 (Azixa), a Microtubule Destabilizing Agent, in Patients with Advanced Cancer

(2010) A.-M. Tsimberidou et al.   MOLECULAR CANCER THERAPEUTICS

Interference with endothelial cell function by JG-03-14, an agent that binds to the colchicine site on microtubules

(2009) Nava Dalyot-Herman et al.   BIOCHEMICAL PHARMACOLOGY

Synthesis and antitumor-evaluation of cyclopropyl-containing combretastatin analogs

(2009) Rita Fürst et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A novel chalcone derivative which acts as a microtubule depolymerising agent and an inhibitor of P-gp and BCRP in in-vitro and in-vivoglioblastoma models

(2009) Ahcene Boumendjel et al.   BMC CANCER

Class III β-tubulin expression and in vitro resistance to microtubule targeting agents

(2009) C Stengel et al.   BRITISH JOURNAL OF CANCER

Novel Microtubule Polymerization Inhibitor with Potent Antiproliferative and Antitumor Activity

(2009) S. Arora et al.   CANCER RESEARCH

Synthesis and Structure-Activity Relationships of 1-Benzyl-4,5,6-trimethoxyindoles as a Novel Class of Potent Antimitotic Agents

(2009) Mei-Jung Lai et al.   ChemMedChem

Activity of 2 methoxyestradiol (Panzem ® NCD) in advanced, platinum-resistant ovarian cancer and primary peritoneal carcinomatosis: A Hoosier Oncology Group trial

(2009) Daniela Matei et al.   GYNECOLOGIC ONCOLOGY

Discovery of 4-Substituted Methoxybenzoyl-aryl-thiazole as Novel Anticancer Agents: Synthesis, Biological Evaluation, and Structure−Activity Relationships

(2009) Yan Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

New Arylthioindoles and Related Bioisosteres at the Sulfur Bridging Group. 4. Synthesis, Tubulin Polymerization, Cell Growth Inhibition, and Molecular Modeling Studies

(2009) Giuseppe La Regina et al.   JOURNAL OF MEDICINAL CHEMISTRY

CYT997: a novel orally active tubulin polymerization inhibitor with potent cytotoxic and vascular disrupting activity in vitro and in vivo

(2009) C. J. Burns et al.   MOLECULAR CANCER THERAPEUTICS

UA62784, a novel inhibitor of centromere protein E kinesin-like protein

(2009) M. C. Henderson et al.   MOLECULAR CANCER THERAPEUTICS

S9, a Novel Anticancer Agent, Exerts Its Anti-Proliferative Activity by Interfering with Both PI3K-Akt-mTOR Signaling and Microtubule Cytoskeleton

(2009) Chao Zhang et al.   PLoS One

Variations in the colchicine-binding domain provide insight into the structural switch of tubulin

(2009) A. Dorleans et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Inhibition of the Ras-Net (Elk-3) Pathway by a Novel Pyrazole that Affects Microtubules

(2008) C. Wasylyk et al.   CANCER RESEARCH

1,2,3,4-Tetrahydro-2-thioxopyrimidine analogs of combretastatin-A4

(2008) Lauren Lee et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Antitumor Activity of New Substituted 3-(5-Imidazo[2,1-b]thiazolylmethylene)-2-indolinones and 3-(5-Imidazo[2,1-b]thiadiazolylmethylene)-2-indolinones: Selectivity against Colon Tumor Cells and Effect on Cell Cycle-Related Events(1)

(2008) Aldo Andreani et al.   JOURNAL OF MEDICINAL CHEMISTRY

Antitumor Agents 260. New Desmosdumotin B Analogues with Improved In Vitro Anticancer Activity

(2008) Kyoko Nakagawa-Goto et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 4-Amino and 4-Hydroxy-1-aroylindoles as Potent Tubulin Polymerization Inhibitors

(2008) Jing-Ping Liou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 2-Chloro-N-(4-methoxyphenyl)-N-methylquinazolin-4-amine (EP128265, MPI-0441138) as a Potent Inducer of Apoptosis with High In Vivo Activity

(2008) Nilantha Sirisoma et al.   JOURNAL OF MEDICINAL CHEMISTRY

New C5-Alkylated Indolobenzazepinones Acting as Inhibitors of Tubulin Polymerization: Cytotoxic and Antitumor Activities

(2008) Laurent Keller et al.   JOURNAL OF MEDICINAL CHEMISTRY

Discovery of 4-Aryl-4H-chromenes as a New Series of Apoptosis Inducers Using a Cell- and Caspase-Based High Throughput Screening Assay. 4. Structure–Activity Relationships ofN-Alkyl Substituted Pyrrole Fused at the 7,8-Positions

(2008) William Kemnitzer et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel A-Ring and B-Ring Modified Combretastatin A-4 (CA-4) Analogues Endowed with Interesting Cytotoxic Activity

(2008) Daniele Simoni et al.   JOURNAL OF MEDICINAL CHEMISTRY

Is class III β-tubulin a predictive factor in patients receiving tubulin-binding agents?

(2008) Pascal Sève et al.   LANCET ONCOLOGY

IRC-083927 is a new tubulin binder that inhibits growth of human tumor cells resistant to standard tubulin-binding agents

(2008) A.-M. Liberatore et al.   MOLECULAR CANCER THERAPEUTICS

Significant antitumor activity in vivo following treatment with the microtubule agent ENMD-1198

(2008) Theresa M. LaVallee et al.   MOLECULAR CANCER THERAPEUTICS

KRIBB3, a novel microtubule inhibitor, induces mitotic arrest and apoptosis in human cancer cells

(2007) Ki Deok Shin et al.   BIOCHEMICAL PHARMACOLOGY

Synthesis and biological evaluation of imidazol-2-one derivatives as potential antitumor agents

(2007) Na Xue et al.   BIOORGANIC & MEDICINAL CHEMISTRY