Recent Advances of Tubulin Inhibitors Targeting the Colchicine Binding Site for Cancer Therapy

Recent Advances in Combretastatin A-4 Inspired Inhibitors of Tubulin Polymerization-An Update

(2022) Sultan Nacak Baytas   CURRENT MEDICINAL CHEMISTRY

Highly Antiproliferative Latonduine and Indolo[2,3-c]quinoline Derivatives: Complex Formation with Copper(II) Markedly Changes the Kinase Inhibitory Profile

(2022) Christopher Wittmann et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, biological assessment, and in-Silico studies of 1,2,4-triazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors

(2022) Heba S. Mohamed et al.   BIOORGANIC CHEMISTRY

Targeting the tumor microenvironment by an enzyme-responsive prodrug of tubulin destabilizer for triple-negative breast cancer therapy with high safety

(2022) Yingyuan Peng et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A Review of the Recent Developments of Molecular Hybrids Targeting Tubulin Polymerization

(2022) Oluwakemi Ebenezer et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Design and synthesis of novel substituted indole-acrylamide derivatives and evaluation of their anti-cancer activity as potential tubulin-targeting agents

(2022) Mohammed Hawash et al.   JOURNAL OF MOLECULAR STRUCTURE

Indole-Based Tubulin Inhibitors: Binding Modes and SARs Investigations

(2022) Sheng Tang et al.   MOLECULES

Synthesis of novel indole‐oxadiazole molecular hybrids by a regioselective C‐3 sulfenylation of indole with 1,3,4‐oxadiazole‐2‐thiols using iodine‐dimethyl sulfoxide and their anticancer properties

(2022) Kartik Dutta et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Domino Semipinacol/Iterative Aldol/Iso-Nazarov Cyclization to Triaryl-cyclopentenone: Enantioselective Synthesis of Combretastatin A-4 Analogues

(2022) Narra Rajashekar Reddy et al.   ORGANIC LETTERS

The Versatile Quinoline and Its Derivatives as anti-Cancer Agents: An Overview

(2022) Basavarajaiah Suliphuldevara Mathada   POLYCYCLIC AROMATIC COMPOUNDS

Synthesis of novel isoxazole–carboxamide derivatives as promising agents for melanoma and targeted nano-emulgel conjugate for improved cellular permeability

(2022) Mohammed Hawash et al.   BMC Chemistry

Discovery of N-benzylarylamide derivatives as novel tubulin polymerization inhibitors capable of activating the Hippo pathway

(2022) Jian Song et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Small-molecule inhibitors, immune checkpoint inhibitors, and more: FDA-approved novel therapeutic drugs for solid tumors from 1991 to 2021

(2022) Qing Wu et al.   Journal of Hematology & Oncology

Synthesis of indole-tetrazole coupled aromatic amides; In vitro anticancer activity, in vitro tubulin polymerization inhibition assay and in silico studies

(2022) T Shreedhar Reddy et al.   JOURNAL OF MOLECULAR STRUCTURE

Evaluation of cytotoxic, COX inhibitory, and antimicrobial activities of novel isoxazole-carboxamide derivatives

(2022) Mohammed Hawash et al.   Letters in Drug Design & Discovery

Design, synthesis and molecular docking study of thiophenyl hydrazone derivatives as tubulin polymerization inhibitors

(2022) Vinutha Kuchana et al.   SYNTHETIC COMMUNICATIONS

Synthesis, Characterisation and Mechanism of Action of Anticancer 3-Fluoroazetidin-2-ones

(2022) Azizah M. Malebari et al.   Pharmaceuticals

Novel combretastatin A-4 derivative containing aminophosphonates as dual inhibitors of tubulin and matrix metalloproteinases for lung cancer treatment

(2022) Xiaochao Huang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, characterization, and anticancer activity of a novel series of O-substituted chalcone derivatives

(2021) Bathélémy Ngameni et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A novel series of benzothiazepine derivatives as tubulin polymerization inhibitors with anti-tumor potency

(2021) Bin Wang et al.   BIOORGANIC CHEMISTRY

Identification of new 3-phenyl-1H-indole-2-carbohydrazide derivatives and their structure-activity relationships as potent tubulin inhibitors and anticancer agents: A combined in silico, in vitro and synthetic study

(2021) Rungroj Saruengkhanphasit et al.   BIOORGANIC CHEMISTRY

Induction of Apoptosis in Hepatocellular Carcinoma Cell Lines by Novel Indolylacrylamide Derivatives: Synthesis and Biological Evaluation

(2021) Mohammed Hawash et al.   CHEMISTRY & BIODIVERSITY

Synthesis and Biological Evaluation of Novel Isoxazole-Amide Analogues as Anticancer and Antioxidant Agents

(2021) Ahmad M. Eid et al.   Biomed Research International

Synthesis and Biological Screening of New Cyano-Substituted Pyrrole Fused (Iso)Quinoline Derivatives

(2021) Maria Cristina Al-Matarneh et al.   MOLECULES

Effect of cabazitaxel on macrophages improves CD47-targeted immunotherapy for triple-negative breast cancer

(2021) Xu Cao et al.   Journal for ImmunoTherapy of Cancer

Design, synthesis and biological evaluation of novel acridine and quinoline derivatives as tubulin polymerization inhibitors with anticancer activities

(2021) Yichang Ren et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of an indole-substituted furanone with tubulin polymerization inhibition activity

(2021) Patricia Mowery et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis and biological evaluation of novel imidazole-chalcone derivatives as potential anticancer agents and tubulin polymerization inhibitors

(2021) Sara Rahimzadeh Oskuei et al.   BIOORGANIC CHEMISTRY

Concise synthesis and biological evaluation of 2-Aryl-3-Anilinobenzo[b]thiophene derivatives as potent apoptosis-inducing agents

(2021) Romeo Romagnoli et al.   BIOORGANIC CHEMISTRY

Design, synthesis and bioevaluation of 6-aryl-1-(3,4,5-trimethoxyphenyl)-1H-benzo[d]imidazoles as tubulin polymerization inhibitors

(2021) Runlai Liu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of highly potent tubulin polymerization inhibitors: Design, synthesis, and structure-activity relationships of novel 2,7-diaryl-[1,2,4]triazolo[1,5-a]pyrimidines

(2021) Xian-Sen Huo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluation of Stable Colchicine-Binding Site Tubulin Inhibitors 6-Aryl-2-benzoyl-pyridines as Potential Anticancer Agents

(2021) Hao Chen et al.   JOURNAL OF MEDICINAL CHEMISTRY

Characterization of gamma-ray and neutron radiation absorption properties of synthesized quinoline derivatives and their genotoxic potential

(2021) Burak Alaylar et al.   RADIATION PHYSICS AND CHEMISTRY

Chalcone Derivatives: Role in Anticancer Therapy

(2021) Yang Ouyang et al.   Biomolecules

Vincristine in Combination Therapy of Cancer: Emerging Trends in Clinics

(2021) Jan Škubník et al.   Biology-Basel

Design, synthesis and evaluation of novel bis-substituted aromatic amide dithiocarbamate derivatives as colchicine site tubulin polymerization inhibitors with potent anticancer activities

(2021) Ya-Xin Sun et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A review on synthetic chalcone derivatives as tubulin polymerisation inhibitors

(2021) Wenjing Liu et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

An Insight into FDA Approved Antibody-Drug Conjugates for Cancer Therapy

(2021) Juliana T. W. Tong et al.   MOLECULES

Synthesis, Biological, and Molecular Docking Studies on 4,5,6,7-Tetrahydrobenzo[b]thiophene Derivatives and Their Nanoparticles Targeting Colorectal Cancer

(2021) Shimaa Kamal et al.   ACS Omega

Synthesis of novel indole-isoxazole hybrids and evaluation of their cytotoxic activities on hepatocellular carcinoma cell lines

(2021) Mohammed Hawash et al.   BMC Chemistry

Design, synthesis, biological evaluation and molecular docking studies of new chalcone derivatives containing diaryl ether moiety as potential anticancer agents and tubulin polymerization inhibitors

(2020) Guangcheng Wang et al.   BIOORGANIC CHEMISTRY

Synthesis and Biological Evaluation of New Antitubulin Agents Containing 2-(3′,4′,5′-trimethoxyanilino)-3,6-disubstituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine Scaffold

(2020) Romeo Romagnoli et al.   MOLECULES

Synthesis and bioevaluation of N-(3,4,5-trimethoxyphenyl)-1H-pyrazolo[3,4-b]pyridin-3-amines as tubulin polymerization inhibitors with anti-angiogenic effects

(2020) Shu-Yi Hao et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of novel indole-based oxalamide and aminoacetamide derivatives as tubulin polymerization inhibitors

(2019) Peng-Cheng Diao et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis, biological evaluation, and molecular modelling of new naphthalene-chalcone derivatives as potential anticancer agents on MCF-7 breast cancer cells by targeting tubulin colchicine binding site

(2019) Guangcheng Wang et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

New thiazole-2(3H)-thiones containing 4-(3,4,5-trimethoxyphenyl) moiety as anticancer agents

(2019) Mahsa Ansari et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Recent advances in CDK inhibitors for cancer therapy

(2018) Amy B Heptinstall et al.   Future Medicinal Chemistry

Global cancer statistics 2018: GLOBOCAN estimates of incidence and mortality worldwide for 36 cancers in 185 countries

(2018) Freddie Bray et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Design, synthesis and biological evaluation of quinoline-indole derivatives as anti-tubulin agents targeting the colchicine binding site

(2018) Wenlong Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of novel pyrazolic chalcone derivatives as novel hepatocellular carcinoma therapeutics

(2017) Mohammed M.A. Hawash et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis and Cytotoxic Evaluation of Novel Chalcone Derivatives Bearing Triazolo[4,3-a]-quinoxaline Moieties as Potent Anticancer Agents with Dual EGFR Kinase and Tubulin Polymerization Inhibitory Effects

(2017) Mohamed Alswah et al.   MOLECULES

Development of Novel Bis(indolyl)-hydrazide–Hydrazone Derivatives as Potent Microtubule-Targeting Cytotoxic Agents against A549 Lung Cancer Cells

(2016) Dipanwita Das Mukherjee et al.   BIOCHEMISTRY

Synthesis and antiviral properties of novel indole-based thiosemicarbazides and 4-thiazolidinones

(2016) Gökçe Cihan-Üstündağ et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Triazole tethered C 5 -curcuminoid-coumarin based molecular hybrids as novel antitubulin agents: Design, synthesis, biological investigation and docking studies

(2016) Harbinder Singh et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, Evaluation, and Mechanism Study of Novel Indole-Chalcone Derivatives Exerting Effective Antitumor Activity Through Microtubule Destabilization in Vitro and in Vivo

(2016) Jun Yan et al.   JOURNAL OF MEDICINAL CHEMISTRY

Potent Antitumor Activities and Structure Basis of the Chiral β-Lactam Bridged Analogue of Combretastatin A-4 Binding to Tubulin

(2016) Pengfei Zhou et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of benzocyclooctene-based and indene-based anticancer agents that function as inhibitors of tubulin polymerization

(2016) Christine A. Herdman et al.   MedChemComm

Combretastatin-A4 phosphate improves the distribution and antitumor efficacy of albumin-bound paclitaxel in W256 breast carcinoma model

(2016) Meng Gao et al.   Oncotarget

A novel synthetic compound exerts effective anti-tumour activity in vivo via the inhibition of tubulin polymerisation in A549 cells

(2015) Jun Yan et al.   BIOCHEMICAL PHARMACOLOGY

Triazole linked mono carbonyl curcumin-isatin bifunctional hybrids as novel anti tubulin agents: Design, synthesis, biological evaluation and molecular modeling studies

(2015) Sahil Sharma et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Microwave-assisted synthesis and biological evaluation of 3,4-diaryl maleic anhydride/N-substituted maleimide derivatives as combretastatin A-4 analogues

(2015) Qi Guan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Antimitotic drugs in the treatment of cancer

(2015) Rustelle Janse van Vuuren et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Combined Molecular Docking, 3D-QSAR, and Pharmacophore Model: Design of Novel Tubulin Polymerization Inhibitors by Binding to Colchicine-binding Site

(2015) Dong-Dong Li et al.   Chemical Biology & Drug Design

A Phase I/II Trial of BNC105P with Everolimus in Metastatic Renal Cell Carcinoma

(2015) S. Pal et al.   CLINICAL CANCER RESEARCH

Design and synthesis of pyrazole–oxindole conjugates targeting tubulin polymerization as new anticancer agents

(2015) Ahmed Kamal et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, biological evaluation and preliminary mechanism study of novel benzothiazole derivatives bearing indole-based moiety as potent antitumor agents

(2015) Junjie Ma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

A review on recent developments of indole-containing antiviral agents

(2015) Ming-Zhi Zhang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

3-Methyl-2-phenyl-1-substituted-indole derivatives as indomethacin analogs: design, synthesis and biological evaluation as potential anti-inflammatory and analgesic agents

(2015) Khaled R. A. Abdellatif et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Synthesis and Biochemical Evaluation of 3-Phenoxy-1,4-diarylazetidin-2-ones as Tubulin-Targeting Antitumor Agents

(2015) Thomas F. Greene et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of pyrazole/isoxazole linked arylcinnamides as tubulin polymerization inhibitors and potential antiproliferative agents

(2015) Ahmed Kamal et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Synthesis of (Z)-(arylamino)-pyrazolyl/isoxazolyl-2-propenones as tubulin targeting anticancer agents and apoptotic inducers

(2015) Ahmed Kamal et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Combretastatin A4-phosphate and its potential in veterinary oncology: a review

(2015) E. Abma et al.   Veterinary and Comparative Oncology

Synthesis and anti-cancer screening of novel heterocyclic-(2H)-1,2,3-triazoles as potential anti-cancer agents

(2015) Narsimha Reddy Penthala et al.   MedChemComm

Synthesis, biological evaluation and molecular docking studies of trans-indole-3-acrylamide derivatives, a new class of tubulin polymerization inhibitors

(2014) Sultan Nacak Baytas et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Chalcone based azacarboline analogues as novel antitubulin agents: Design, synthesis, biological evaluation and molecular modelling studies

(2014) Sahil Sharma et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of azaisoerianin derivatives as potential antitumors agents

(2014) Mohamed Ali Soussi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

β-Lactam Estrogen Receptor Antagonists and a Dual-Targeting Estrogen Receptor/Tubulin Ligand

(2014) Niamh M. O’Boyle et al.   JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Biological Evaluation of Stable Colchicine Binding Site Tubulin Inhibitors as Potential Anticancer Agents

(2014) Yan Lu et al.   JOURNAL OF MEDICINAL CHEMISTRY

Tubulin Inhibitors: A Patent Survey

(2014) Kunal Nepali et al.   Recent Patents on Anti-Cancer Drug Discovery

Synthesis of combretastatin A-4 O-alkyl derivatives and evaluation of their cytotoxic, antiangiogenic and antitelomerase activity

(2013) Sandra Torijano-Gutiérrez et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Design and synthesis of silicon-containing tubulin polymerization inhibitors: Replacement of the ethylene moiety of combretastatin A-4 with a silicon linker

(2013) Masaharu Nakamura et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and evaluation of diaryl sulfides and diaryl selenide compounds for antitubulin and cytotoxic activity

(2013) Edson dos A. dos Santos et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A Concise Synthesis of Pyrazole Analogues of Combretastatin A1 as Potent Anti-Tubulin Agents

(2013) Roberta Zaninetti et al.   ChemMedChem

Design, synthesis and anticancer properties of 5-arylbenzoxepins as conformationally restricted iso combretastatin A-4 analogs

(2013) Evelia Rasolofonjatovo et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Concise Synthesis and Biological Evaluation of 2-Aroyl-5-Amino Benzo[b]thiophene Derivatives As a Novel Class of Potent Antimitotic Agents

(2013) Romeo Romagnoli et al.   JOURNAL OF MEDICINAL CHEMISTRY

Endowing Indole-Based Tubulin Inhibitors with an Anchor for Derivatization: Highly Potent 3-Substituted Indolephenstatins and Indoleisocombretastatins

(2013) Raquel Álvarez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Biological Evaluation of 2-(Alkoxycarbonyl)-3-Anilinobenzo[b]thiophenes and Thieno[2,3-b]pyridines as New Potent Anticancer Agents

(2013) Romeo Romagnoli et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, cytotoxicity, and molecular properties prediction of novel 1,3-diarylpyrazole derivatives

(2013) Sultan Nacak Baytas et al.   MEDICINAL CHEMISTRY RESEARCH

Antimitotic Chalcones and Related Compounds as Inhibitors of Tubulin Assembly

(2012) Sylvie Ducki   Anti-Cancer Agents in Medicinal Chemistry

Synthesis and biological evaluation of 2-substituted-4-(3′,4′,5′-trimethoxyphenyl)-5-aryl thiazoles as anticancer agents

(2012) Romeo Romagnoli et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Phase I Trial of Combretastatin A4 Phosphate (CA4P) in Combination with Bevacizumab in Patients with Advanced Cancer

(2012) P. Nathan et al.   CLINICAL CANCER RESEARCH

In vitro and in vivo biological evaluation of new 4,5-disubstituted 1,2,3-triazoles as cis-constrained analogs of combretastatin A4

(2012) Núria Mur Blanch et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

US Food and Drug Administration Approval Overview in Metastatic Breast Cancer

(2012) Patricia Cortazar et al.   JOURNAL OF CLINICAL ONCOLOGY

Toward Highly Potent Cancer Agents by Modulating the C-2 Group of the Arylthioindole Class of Tubulin Polymerization Inhibitors

(2012) Giuseppe La Regina et al.   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

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

Targeted delivery of a combination therapy consisting of combretastatin A4 and low-dose doxorubicin against tumor neovasculature

(2011) Tingyuan Yang et al.   Nanomedicine-Nanotechnology Biology and Medicine

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

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

Phenylcinnamides as Novel Antimitotic Agents

(2010) Benjamin J. Leslie 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

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

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

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