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

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

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

Chemometric analysis of bio-inspired micellar electrokinetic chromatographic systems – modelling of retention mechanism and prediction of biological properties using bile salts surfactants

(2021) Krzesimir Ciura et al.   MICROCHEMICAL JOURNAL

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

BF3-promoted annulation of azonaphthalenes and ynamides for synthesis of benzo[e]indoles

(2020) Changwei Chen et al.   CHINESE CHEMICAL LETTERS

Recent Trends in Drug Design and Discovery

(2020) D. Velmurugan et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Inorganic nanoparticles for natural product delivery: a review

(2020) Jairam Meena et al.   Environmental Chemistry Letters

Synthesis and Preclinical Evaluation of Indole Triazole Conjugates as Microtubule Targeting Agents that are Effective against MCF-7 Breast Cancer Cell Lines

(2020) Vidyasrilekha Yele et al.   Anti-Cancer Agents in Medicinal Chemistry

The effect of drug position on the properties of paclitaxel-conjugated gold nanoparticles for liver tumor treatment

(2020) Huaisong Wang et al.   CHINESE CHEMICAL LETTERS

Synergistic in-situ growth of silver nanoparticles with nanozyme activity for dual-mode biosensing and cancer theranostics

(2020) Xin Hai et al.   CHINESE CHEMICAL LETTERS

Prodrugs: My Initial Exploration and Where It Led

(2020) Valentino J. Stella   JOURNAL OF PHARMACEUTICAL SCIENCES

Synthesis, anticancer and antioxidant properties of new indole and pyranoindole derivatives

(2020) Domenico Iacopetta et al.   BIOORGANIC 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, synthesis and biological evaluation of vinyl selenone derivatives as novel microtubule polymerization inhibitors

(2020) Huajian Zhu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Recent advances in ionic liquids and nanotechnology for drug delivery

(2020) Mariana Amaral et al.   Nanomedicine

Synthesis of polycyclic spiro-fused indolines via IBX-mediated cascade cyclization

(2020) Zhiguo Zhang et al.   CHINESE CHEMICAL LETTERS

Quinolone hybrids and their anti-cancer activities: An overview

(2019) Feng Gao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Discover 4β-NH-(6-aminoindole)-4-desoxy-podophyllotoxin with nanomolar-potency antitumor activity by improving the tubulin binding affinity on the basis of a potential binding site nearby colchicine domain

(2019) Wei Zhao et al.   EUROPEAN JOURNAL OF MEDICINAL 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

A supramolecular co-delivery strategy for combined breast cancer treatment and metastasis prevention

(2019) Yuxuan Chen et al.   CHINESE CHEMICAL LETTERS

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

A drug-likeness toolbox facilitates ADMET study in drug discovery

(2019) Chen-Yang Jia et al.   DRUG DISCOVERY TODAY

Organocatalytic Asymmetric Synthesis of Indole-Based Chiral Heterocycles: Strategies, Reactions, and Outreach

(2019) Yu-Chen Zhang et al.   ACCOUNTS OF CHEMICAL RESEARCH

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

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

N -Arylsulfonylsubstituted- 1H indole derivatives as small molecule dual inhibitors of signal transducer and activator of transcription 3 (STAT3) and tubulin

(2018) Qiang Zhou et al.   BIOORGANIC & 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

Design, synthesis and biological evaluation of 1, 4-dihydro indeno[1,2- c ] pyrazole linked oxindole analogues as potential anticancer agents targeting tubulin and inducing p53 dependent apoptosis

(2018) Irfan Khan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel nicotinoyl pyrazoline derivates bearing N-methyl indole moiety as antitumor agents: Design, synthesis and evaluation

(2018) Kun Chen 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

Discovery of novel vinyl sulfone derivatives as anti-tumor agents with microtubule polymerization inhibitory and vascular disrupting activities

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

Design, synthesis, in vitro antiproliferative activity and apoptosis-inducing studies of 1-(3′,4′,5′-trimethoxyphenyl)-3-(2′-alkoxycarbonylindolyl)-2-propen-1-one derivatives obtained by a molecular hybridisation approach

(2018) Delia Preti et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Research advances on anticancer activities of matrine and its derivatives: An updated overview

(2018) Haroon ur Rashid et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

1-Arylsulfonyl indoline-benzamides as a new antitubulin agents, with inhibition of histone deacetylase

(2018) Mei-Jung Lai et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, biological evaluation, and molecular docking investigation of 3-amidoindoles as potent tubulin polymerization inhibitors

(2018) Peng Chen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

Synthesis and biological evaluation of curcumin inspired indole analogues as tubulin polymerization inhibitors

(2017) P.V. Sri Ramya et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of C 5 -tethered indolyl-3-glyoxylamide derivatives as tubulin polymerization inhibitors

(2017) Sravanthi Devi Guggilapu et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design and synthesis of bis(indolyl)ketohydrazide-hydrazones: Identification of potent and selective novel tubulin inhibitors

(2017) Mukund P. Tantak et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and biological evaluation of novel indole-pyrimidine hybrids bearing morpholine and thiomorpholine moieties

(2017) Peng-Cheng Diao et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, and biological evaluation of cyclic-indole derivatives as anti-tumor agents via the inhibition of tubulin polymerization

(2017) Jun Yan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and evaluation of selenium-containing indole chalcone and diarylketone derivatives as tubulin polymerization inhibition agents

(2017) Shun Zhang et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Discovery and Optimization of Novel 5-Indolyl-7-arylimidazo[1,2-a]pyridine-8-carbonitrile Derivatives as Potent Antitubulin Agents Targeting Colchicine-binding Site

(2017) Xin Zhai et al.   Scientific Reports

Synthesis and Biological Evaluation of 1-Methyl-1H-indole-Pyrazoline Hybrids as Potential Tubulin Polymerization Inhibitors

(2016) Ya-Liang Zhang et al.   ChemMedChem

Recent advances of cytotoxic chalconoids targeting tubulin polymerization: Synthesis and biological activity

(2016) Hassan Mirzaei et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Indoles — A promising scaffold for drug development

(2016) T.V. Sravanthi et al.   EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

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

Novel Natural Product- and Privileged Scaffold-Based Tubulin Inhibitors Targeting the Colchicine Binding Site

(2016) Mengqi Dong et al.   MOLECULES

Synthesis and biological evaluation of novel indole derivatives containing sulfonamide scaffold as potential tubulin inhibitor

(2016) Ruo-Jun Man et al.   MedChemComm

Microwave-assisted synthesis of 3-sulfenylindoles by sulfonyl hydrazides using organic ionic base-Brønsted acid

(2016) Rajjakfur Rahaman et al.   RSC Advances

Design, Synthesis and Antitumor Activity of Novel link-bridge and B-Ring Modified Combretastatin A-4 (CA-4) Analogues as Potent Antitubulin Agents

(2016) Yong-Tao Duan et al.   Scientific Reports

Synthesis and biological evaluation of benzimidazole–oxindole conjugates as microtubule-targeting agents

(2015) Ahmed Kamal et al.   BIOORGANIC CHEMISTRY

Design, Synthesis and Molecular Docking Studies of Novel Indole-Pyrimidine Hybrids as Tubulin Polymerization Inhibitors

(2015) Meng-Jin Hu et al.   Chemical Biology & Drug Design

Heterocyclic Scaffolds: Centrality in Anticancer Drug Development

(2015) Imran Ali et al.   CURRENT DRUG TARGETS

Synthesis, biological evaluation, and molecular docking studies of novel 1-benzene acyl-2-(1-methylindol-3-yl)-benzimidazole derivatives as potential tubulin polymerization inhibitors

(2015) Yan-Ting Wang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

3-(3,4,5-Trimethoxyphenylselenyl)-1H-indoles and their selenoxides as combretastatin A-4 analogs: Microwave-assisted synthesis and biological evaluation

(2015) Zhiyong Wen et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

New Indole Tubulin Assembly Inhibitors Cause Stable Arrest of Mitotic Progression, Enhanced Stimulation of Natural Killer Cell Cytotoxic Activity, and Repression of Hedgehog-Dependent Cancer

(2015) Giuseppe La Regina et al.   JOURNAL OF MEDICINAL CHEMISTRY

An Orally Bioavailable, Indole-3-glyoxylamide Based Series of Tubulin Polymerization Inhibitors Showing Tumor Growth Inhibition in a Mouse Xenograft Model of Head and Neck Cancer

(2015) Helen E. Colley et al.   JOURNAL OF MEDICINAL CHEMISTRY

Novel 2-Carbonylbenzo[b]thiophene 1,1-Dioxide Derivatives as Potent Inhibitors of STAT3 Signaling Pathway

(2015) Peng Ji et al.   ACS Medicinal Chemistry Letters

IPP51, a chalcone acting as a microtubule inhibitor with in vivo antitumor activity against bladder carcinoma

(2015) Véronique Martel-Frachet et al.   Oncotarget

Design, synthesis and biological evaluation of a series of pyrano chalcone derivatives containing indole moiety as novel anti-tubulin agents

(2014) Guangcheng Wang et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

Recent developments in tubulin polymerization inhibitors: An overview

(2014) Ramandeep Kaur et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery and molecular modeling of novel 1-indolyl acetate – 5-Nitroimidazole targeting tubulin polymerization as antiproliferative agents

(2014) Yong-Tao Duan et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and evaluation of benzimidazole carbamates bearing indole moieties for antiproliferative and antitubulin activities

(2014) Qi Guan et al.   EUROPEAN 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

A Scalable One-Pot Process for the Synthesis of Florfenicol Phosphodiester

(2014) Shuang-Xi Gu et al.   ORGANIC PROCESS RESEARCH & DEVELOPMENT

Synthesis and biological evaluation of indole-based, anti-cancer agents inspired by the vascular disrupting agent 2-(3′-hydroxy-4′-methoxyphenyl)-3-(3″,4″,5″-trimethoxybenzoyl)-6-methoxyindole (OXi8006)

(2013) Matthew T. MacDonough et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis and Biological Evaluation of Imidazopyridine-Oxindole Conjugates as Microtubule-Targeting Agents

(2013) Ahmed Kamal et al.   ChemMedChem

Synthesis of a 2-Aryl-3-aroyl Indole Salt (OXi8007) Resembling Combretastatin A-4 with Application as a Vascular Disrupting Agent

(2013) Mallinath B. Hadimani et al.   JOURNAL OF NATURAL PRODUCTS

Interference of a novel indolylmaleimide with microtubules induces mitotic arrest and apoptosis in human progenitor and cancer cells

(2012) Christian Eisenlöffel et al.   BIOCHEMICAL PHARMACOLOGY

2-Arylindoles: A Privileged Molecular Scaffold with Potent, Broad-Ranging Pharmacological Activity

(2012) S. Lal et al.   CURRENT MEDICINAL CHEMISTRY

Design and synthesis of biaryl aryl stilbenes/ethylenes as antimicrotubule agents

(2012) A. Suresh Kumar et al.   EUROPEAN 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

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

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

Methylselenol, a selenium metabolite, modulates p53 pathway and inhibits the growth of colon cancer xenografts in Balb/c mice

(2012) Huawei Zeng et al.   JOURNAL OF NUTRITIONAL BIOCHEMISTRY

Synthesis, anticancer activity and apoptosis inducing ability of bisindole linked pyrrolo[2,1-c][1,4]benzodiazepine conjugates

(2011) Ahmed Kamal et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Global cancer statistics

(2011) Ahmedin Jemal et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Melanoma Prevention Using Topical PBISe

(2011) C.-Y. Chung et al.   Cancer Prevention Research

Advanced Drug Delivery Systems of Curcumin for Cancer Chemoprevention

(2011) S. S. Bansal et al.   Cancer Prevention Research

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

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

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

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

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

Concise syntheses of N-aryl-5,6,7-trimethoxyindoles as antimitotic and vascular disrupting agents: application of the copper-mediated Ullmann-type arylation

(2011) Hsueh-Yun Lee et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Investigation of a new 1,3-diarylpropenone as a potential antimitotic agent targeting bladder carcinoma

(2010) Véronique Martel-Frachet et al.   ANTI-CANCER DRUGS

Synthesis and biological evaluation of indolyl chalcones as antitumor agents

(2010) Dalip Kumar et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Synthesis of Anti-Microtubule N-(2-Arylindol-7-yl)benzenesulfonamide Derivatives and Their Antitumor Mechanisms

(2010) Chun-Tang Chiou et al.   ChemMedChem

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

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

Microtubule-binding agents: a dynamic field of cancer therapeutics

(2010) Charles Dumontet et al.   NATURE REVIEWS DRUG DISCOVERY

The use of anhydrous CeCl3 as a catalyst for the synthesis of 3-sulfenyl indoles

(2010) Claudio C. Silveira et al.   TETRAHEDRON LETTERS

The selenium to selenoprotein pathway in eukaryotes: More molecular partners than anticipated

(2009) Christine Allmang et al.   BIOCHIMICA ET BIOPHYSICA ACTA-GENERAL SUBJECTS

Antioxidant activity of 5,10-dihydroindeno[1,2-b]indoles containing substituents on dihydroindeno part

(2009) Oktay Talaz et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Synthesis, in vitro structure–activity relationship, and in vivo studies of 2-arylthiazolidine-4-carboxylic acid amides as anticancer agents

(2009) Yan Lu et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

From Nature to Drug Discovery: The Indole Scaffold as a ‘Privileged Structure’

(2009) Fernando de Sa Alves et al.   MINI-REVIEWS IN MEDICINAL CHEMISTRY

Synthesis and biological evaluation of novel 2,4,5-substituted pyrimidine derivatives for anticancer activity

(2008) Fuchun Xie et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2008) A. Wienecke et al.   CANCER RESEARCH

Curcumin: From ancient medicine to current clinical trials

(2008) H. Hatcher et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

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