Indole derivatives targeting colchicine binding site as potential anticancer agents

Identification of novel non-toxic and anti-angiogenic α-fluorinated chalcones as potent colchicine binding site inhibitors

(2022) Moran Sun et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Angiogenesis and anti-leukaemia activity of novel indole derivatives as potent colchicine binding site inhibitors

(2022) Yongfang Yao et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Design, synthesis, characterization and cytotoxic activity of new ortho-hydroxy and indole-chalcone derivatives against breast cancer cells (MCF-7)

(2022) Maadh Jumaah et al.   MEDICINAL CHEMISTRY RESEARCH

Biphasic dose‐dependent G0/G1 and G2/M cell cycle arrest by synthetic 2,3‐arylpyridylindole derivatives in A549 lung cancer cells

(2022) Pongtai Chaiputtanapun et al.   ChemMedChem

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

Target-based anticancer indole derivatives and insight into structure‒activity relationship: A mechanistic review update (2018–2021)

(2022) Ashima Dhiman et al.   Acta Pharmaceutica Sinica B

Discovery of novel coumarin-indole derivatives as tubulin polymerization inhibitors with potent anti-gastric cancer activities

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

Antiproliferative Potential of Gloriosine: A Lead for Anticancer Drug Development

(2022) Bharat Goel et al.   ACS Omega

One-Pot Modified Madelung Synthesis of 3-Tosyl- and 3-Cyano-1,2-disubstituted Indoles

(2022) Grigorii K. Sterligov et al.   ACS Omega

Design, synthesis, and bioevaluation of imidazo [1,2–a] pyrazine derivatives as tubulin polymerization inhibitors with potent anticancer activities

(2022) Bulian Deng et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Discovery of pyrazole‐carbohydrazide with indole moiety as tubulin polymerization inhibitors and anti‐tumor candidates

(2022) Ruo‐Jun Man et al.   DRUG DEVELOPMENT RESEARCH

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

(2022) Mohammed Hawash   Biomolecules

Synthesis and Anticancer Evaluation of Novel Indole Based Arylsulfonylhydrazides against Human Breast Cancer Cells

(2022) Aysha Gaur et al.   ACS Omega

Quinolines, a perpetual, multipurpose scaffold in medicinal chemistry

(2021) Pratibha Yadav 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

Discovery of novel indole‐1,2,4‐triazole derivatives as tubulin polymerization inhibitors

(2021) Meng‐Ke Wu et al.   DRUG DEVELOPMENT RESEARCH

Indolyl-α-keto-1,3,4-oxadiazoles: Synthesis, anti-cell proliferation activity, and inhibition of tubulin polymerization

(2021) Mukund P. Tantak et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Anticancer Potential of Small‐Molecule Inhibitors of Fatty Acid Amide Hydrolase and Monoacylglycerol Lipase

(2021) Shivani Jaiswal et al.   ChemMedChem

Discovery of indoline derivatives as anticancer agents via inhibition of tubulin polymerization

(2021) Shu-Yu Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Indole derivatives (2010–2020) as versatile tubulin inhibitors: synthesis and structure-activity relationships

(2021) Fatima Naaz et al.   Future Medicinal Chemistry

Indole derivatives as tubulin polymerization inhibitors for the development of promising anticancer agents

(2021) Yu Hong et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Molecular interactions at the colchicine binding site in tubulin: An X-ray crystallography perspective

(2021) Jiaxing Wang et al.   DRUG DISCOVERY TODAY

Structure modification and biological evaluation of indole-chalcone derivatives as anti-tumor agents through dual targeting tubulin and TrxR

(2021) Jun Yan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Anticancer properties of indole derivatives as IsoCombretastatin A-4 analogues

(2021) Shannon Pecnard et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of indole-based [1,2,4]triazolo[4,3-a] pyridine derivatives as novel microtubule polymerization inhibitors

(2021) Cheng-Jun Wu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis and biological evaluation of novel 2-phenyl-4,5,6,7-tetrahydro-1H-​indole derivatives as potential anticancer agents and tubulin polymerization inhibitors

(2021) Guangcheng Wang et al.   Arabian Journal of Chemistry

New Multi-Targeted Antiproliferative Agents: Design and Synthesis of IC261-Based Oxindoles as Potential Tubulin, CK1 and EGFR Inhibitors

(2021) Momen R. Fareed et al.   Pharmaceuticals

Design, synthesis and biological evaluation of 2-alkoxycarbonyl-3-anilinoindoles as a new class of potent inhibitors of tubulin polymerization

(2020) Romeo Romagnoli et al.   BIOORGANIC CHEMISTRY

Chalcone hybrids as potential anticancer agents: Current development, mechanism of action, and structure‐activity relationship

(2020) Feng Gao et al.   MEDICINAL RESEARCH REVIEWS

Design, synthesis, and bioevaluation of pyrazolo[1,5-a]pyrimidine derivatives as tubulin polymerization inhibitors targeting the colchicine binding site with potent anticancer activities

(2020) Gang Li et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, biological evaluation, and molecular docking analysis of phenstatin based indole linked chalcones as anticancer agents and tubulin polymerization inhibitors

(2020) Jyoti Kode et al.   BIOORGANIC CHEMISTRY

Design and synthesis of novel cytotoxic indole-thiosemicarbazone derivatives: biological evaluation and docking study

(2019) lotfoallah saghaie et al.   CHEMISTRY & BIODIVERSITY

Revisiting microtubule targeting agents: α-Tubulin and the pironetin binding site as unexplored targets for cancer therapeutics

(2019) Sara K. Coulup et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis and Biological Evaluation of Indole-2-carbohydrazides and Thiazolidinyl-indole-2-carboxamides as Potent Tubulin Polymerization Inhibitors

(2019) Fusun Kazan et al.   COMPUTATIONAL BIOLOGY AND CHEMISTRY

First Report on 3‐(3‐oxoaryl) Indole Derivatives as Anticancer Agents: Microwave Assisted Synthesis, In Vitro Screening and Molecular Docking Studies

(2019) Tarun Patel et al.   ChemistrySelect

Synthesis, Anticancer Activity and Molecular Modeling Studies of Novel Chalcone Derivatives Containing Indole and Naphthalene Moieties as Tubulin Polymerization Inhibitors

(2019) Guangcheng Wang et al.   CHEMICAL & PHARMACEUTICAL BULLETIN

Structure-Guided Design, Synthesis, and Biological Evaluation of (2-(1H-Indol-3-yl)-1H-imidazol-4-yl)(3,4,5-trimethoxyphenyl) Methanone (ABI-231) Analogues Targeting the Colchicine Binding Site in Tubulin

(2019) Qinghui Wang et al.   JOURNAL OF 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

Discovery of certain benzyl/phenethyl thiazolidinone-indole hybrids as potential anti-proliferative agents: Synthesis, molecular modeling and tubulin polymerization inhibition study

(2019) Dilep Kumar Sigalapalli et al.   BIOORGANIC CHEMISTRY

Tubulin: Structure, Functions and Roles in Disease

(2019) Pavla Binarová et al.   Cells

A synthetic 2,3-diarylindole induces microtubule destabilization and G2/M cell cycle arrest in lung cancer cells

(2019) Bongkotrat Thanaussavadate et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Indole: A privileged scaffold for the design of anti-cancer agents

(2019) Yichao Wan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Indirubin, a bis-indole alkaloid binds to tubulin and exhibits antimitotic activity against HeLa cells in synergism with vinblastine

(2018) Lakshmi Mohan et al.   BIOMEDICINE & PHARMACOTHERAPY

Recent advances in trimethoxyphenyl (TMP) based tubulin inhibitors targeting the colchicine binding site

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

Indole in the target-based design of anticancer agents: A versatile scaffold with diverse mechanisms

(2018) Sakineh Dadashpour et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

New 6- and 7-heterocyclyl-1 H -indole derivatives as potent tubulin assembly and cancer cell growth inhibitors

(2018) Giuseppe La Regina et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

1,2,3-triazole tethered Indole-3-glyoxamide derivatives as multiple inhibitors of 5-LOX, COX-2 & tubulin: Their anti-proliferative & anti-inflammatory activity

(2018) Fatima Naaz et al.   BIOORGANIC CHEMISTRY

Design, synthesis and biological evaluation of a novel library of antimitotic C2-aroyl/arylimino tryptamine derivatives that are also potent inhibitors of indoleamine-2, 3-dioxygenase (IDO)

(2018) Jyoti Chauhan et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

An Indole–Chalcone Inhibits Multidrug-Resistant Cancer Cell Growth by Targeting Microtubules

(2018) Hui Cong et al.   MOLECULAR PHARMACEUTICS

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, molecular properties prediction and biological evaluation of indole-vinyl sulfone derivatives as novel tubulin polymerization inhibitors targeting the colchicine binding site

(2018) Wenlong Li et al.   BIOORGANIC CHEMISTRY

Tubulin inhibitors targeting the colchicine binding site: a perspective of privileged structures

(2017) Wenlong Li et al.   Future Medicinal Chemistry

A synthetic 2,3-diarylindole induces cell death via apoptosis and autophagy in A549 lung cancer cells

(2016) Thanya Rukkijakan et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

ST-11: A New Brain-Penetrant Microtubule-Destabilizing Agent with Therapeutic Potential for Glioblastoma Multiforme

(2016) A. E. Cherry et al.   MOLECULAR CANCER THERAPEUTICS

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

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

Discovery of Novel 2-Aryl-4-benzoyl-imidazole (ABI-III) Analogues Targeting Tubulin Polymerization As Antiproliferative Agents

(2012) Jianjun Chen 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

Isocombretastatins A versus Combretastatins A: The ForgottenisoCA-4 Isomer as a Highly Promising Cytotoxic and Antitubulin Agent

(2009) Samir Messaoudi et al.   JOURNAL OF MEDICINAL CHEMISTRY

Microtubule inhibitors: Differentiating tubulin-inhibiting agents based on mechanisms of action, clinical activity, and resistance

(2009) E. A. Perez   MOLECULAR CANCER THERAPEUTICS

Indibulin, a Novel Microtubule Inhibitor, Discriminates between Mature Neuronal and Nonneuronal Tubulin

(2008) A. Wienecke et al.   CANCER RESEARCH

Microtubules: A dynamic target in cancer therapy

(2008) Eddy Pasquier et al.   IUBMB LIFE

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

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