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

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

Discovery of Novel Benzimidazole and Indazole Analogues as Tubulin Polymerization Inhibitors with Potent Anticancer Activities

(2021) Yichang Ren et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of 1,4-dihydropyrazolo[4,3-b]indoles via intramolecular C(sp2)-N bond formation involving nitrene insertion, DFT study and their anticancer assessment

(2021) Manpreet Kaur et al.   BIOORGANIC CHEMISTRY

Morpholine as ubiquitous pharmacophore in medicinal chemistry: Deep insight into the structure-activity relationship (SAR)

(2020) Archana Kumari et al.   BIOORGANIC CHEMISTRY

Imidazo[2,1-b] [1,3,4]thiadiazoles with antiproliferative activity against primary and gemcitabine-resistant pancreatic cancer cells

(2020) Stella Cascioferro et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, Antiproliferative Effect, and Topoisomerase II Inhibitory Activity of 3-Methyl-2-phenyl-1H-indoles

(2020) Nace Zidar et al.   ACS Medicinal Chemistry Letters

New Isatin–Indole Conjugates: Synthesis, Characterization, and a Plausible Mechanism of Their in vitro Antiproliferative Activity

(2020) Reem I. Al-Wabli et al.   Drug Design Development and Therapy

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

Synthesis and biological evaluation of novel pyrazoline derivatives containing indole skeleton as anti-cancer agents targeting topoisomerase II

(2020) Yali Song et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, Synthesis, and Anticancer Evaluation of Novel Indole Derivatives of Ursolic Acid as Potential Topoisomerase II Inhibitors

(2020) A-Liang Li et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Synthesis, Biological Evaluation and In Silico Studies of Certain Oxindole–Indole Conjugates as Anticancer CDK Inhibitors

(2020) Tarfah Al-Warhi et al.   MOLECULES

A review on progression of epidermal growth factor receptor (EGFR) inhibitors as an efficient approach in cancer targeted therapy

(2020) Adileh Ayati et al.   BIOORGANIC CHEMISTRY

Design, synthesis and anticancer/antiestrogenic activities of novel indole-benzimidazoles

(2020) Fikriye Zengin Karadayi et al.   BIOORGANIC CHEMISTRY

Design, synthesis and biological evaluation of some new 2-Pyrazoline derivatives as potential anticancer agents

(2020) Fatih Tok et al.   BIOORGANIC CHEMISTRY

Targeting topoisomerase II with trypthantrin derivatives: Discovery of 7-((2-(dimethylamino)ethyl)amino)indolo[2,1-b]quinazoline-6,12-dione as an antiproliferative agent and to treat cancer

(2020) Elena Catanzaro et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The importance of indole and azaindole scaffold in the development of antitumor agents

(2020) Yu Han et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Indole Curcumin Reverses Multidrug Resistance by Reducing the Expression of ABCB1 and COX2 in Induced Multidrug Resistant Human Lung Cancer Cells

(2020) Sankar Pajaniradje et al.   Letters in Drug Design & Discovery

Discovery of novel indolyl-1,2,4-triazole hybrids as potent vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors with potential anti-renal cancer activity

(2020) Sami A. Al-Hussain 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

Cyclic bridged analogs of isoCA-4: Design, synthesis and biological evaluation

(2020) Shannon Pecnard et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Regulation of apoptosis in health and disease: the balancing act of BCL-2 family proteins

(2019) Rumani Singh et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

Anti-cancer, anti-oxidant and molecular docking studies of thiosemicarbazone indole-based derivatives

(2019) Zohreh Bakherad et al.   RESEARCH ON CHEMICAL INTERMEDIATES

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

(2019) lotfoallah saghaie et al.   CHEMISTRY & BIODIVERSITY

Artemisinin-indole and artemisinin-imidazole hybrids: Synthesis, cytotoxic evaluation and reversal effects on multidrug resistance in MCF-7/ADR cells

(2019) Yanping Hu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Design, synthesis, molecular docking and biological activity evaluation of some novel indole derivatives as potent anticancer active agents and apoptosis inducers

(2019) Ahmed M. Sh. El-Sharief et al.   BIOORGANIC CHEMISTRY

Indole derivatives as multifunctional drugs: Synthesis and evaluation of antioxidant, photoprotective and antiproliferative activity of indole hydrazones

(2019) Monica Demurtas et al.   BIOORGANIC CHEMISTRY

N,N-bis-heteroaryl methylamines: Potent anti-mitotic and highly cytotoxic agents

(2019) Ilhem Khelifi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Revealing quinquennial anticancer journey of morpholine: A SAR based review

(2019) Fatima Arshad et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and Cytotoxicity Evaluation of Novel Indole Derivatives as Potential Anti-Cancer Agents

(2019) Mona Monir Kamel et al.   Medicinal Chemistry

Biological Evaluation of the Antiproliferative and Anti-migratory Activity of a Series of 3-(6-Phenylimidazo[2,1-b][1,3,4]thiadiazol-2-yl)-1H-indole Derivatives Against Pancreatic Cancer Cells

(2019) GIOVANNA LI PETRI et al.   ANTICANCER RESEARCH

Facile one-pot synthesis, antiproliferative evaluation and structure-activity relationships of 3-amino-1H-indoles and 3-amino-1H-7-azaindoles

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

Targeting Topoisomerase I in the Era of Precision Medicine

(2019) Anish Thomas et al.   CLINICAL CANCER RESEARCH

Synthesis and evaluation of 2-carboxy indole derivatives as potent and selective anti-leukemic agents

(2019) Nathália Moreno Cury et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Protein–ligand interaction-guided discovery of novel VEGFR-2 inhibitors

(2019) Yanmin Zhang et al.   JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS

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

Combination therapies of Artemisinin and its derivatives as a viable approach for future cancer treatment

(2019) Maushmi S. Kumar et al.   CURRENT PHARMACEUTICAL DESIGN

Estrogen signaling: An emanating therapeutic target for breast cancer treatment

(2019) Tanmay Saha et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

The tetrahydroxanthone-dimer phomoxanthone A is a strong inducer of apoptosis in cisplatin-resistant solid cancer cells

(2019) Chenyin Wang 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

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

Anticancer Indole-Based Chalcones: A Structural and Theoretical Analysis

(2019) Farid A. Badria et al.   MOLECULES

Amide derivatives of 4-azaindole: Design, synthesis, and EGFR targeting anticancer agents

(2019) Puli Venkat Swamy et al.   SYNTHETIC COMMUNICATIONS

Therapeutic Inducers of Apoptosis in Ovarian Cancer

(2019) Mudra Binju et al.   Cancers

Synthesis and biological evaluation of novel indole-pyrazoline hybrid derivatives as potential topoisomerase 1 inhibitors

(2019) Bing Shu et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

Bisindolemethane derivatives as highly potent anticancer agents: Synthesis, medicinal activity evaluation, cell-based compound discovery, and computational target predictions

(2019) Ashish Bahuguna et al.   COMPUTERS IN BIOLOGY AND MEDICINE

Synthesis, biological evaluation, and docking study of indole aryl sulfonamides as aromatase inhibitors

(2019) Marialuigia Fantacuzzi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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

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

Design, synthesis and biological evaluation of indole-2-carboxylic acid derivatives as IDO1/TDO dual inhibitors

(2019) Guonan Cui et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Keteniminium Salts: Reactivity and Propensity toward Electrocyclization Reactions

(2019) Gamze Tanriver et al.   JOURNAL OF ORGANIC CHEMISTRY

Therapeutic journery of nitrogen mustard as alkylating anticancer agents: Historic to future perspectives

(2018) Rajesh K. Singh 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

Benzofuran hydrazones as potential scaffold in the development of multifunctional drugs: Synthesis and evaluation of antioxidant, photoprotective and antiproliferative activity

(2018) Anna Baldisserotto et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Discovery of the cancer cell selective dual acting anti-cancer agent ( Z )-2-(1 H -indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131)

(2018) Cheng Shang See et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Design, synthesis, antiproliferative activity, molecular docking and cell cycle analysis of some novel (morpholinosulfonyl) isatins with potential EGFR inhibitory activity

(2018) Yousry A. Ammar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Novel [(3-indolylmethylene)hydrazono]indolin-2-ones as apoptotic anti-proliferative agents: design, synthesis and in vitro biological evaluation

(2018) Wagdy M. Eldehna et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

Copper-Catalyzed Synthesis of Multisubstituted Indoles through Tandem Ullmann-Type C–N Formation and Cross-dehydrogenative Coupling Reactions

(2018) Yue Li et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthesis of 2-Acylindoles via Ag- and Cu-Catalyzed anti-Michael Hydroamination of β-(2-Aminophenyl)-α,β-ynones: Experimental Results and DFT Calculations

(2018) Navnath D. Rode et al.   JOURNAL OF ORGANIC CHEMISTRY

One-Pot Synthesis of Indole-3-acetic Acid Derivatives through the Cascade Tsuji–Trost Reaction and Heck Coupling

(2018) Dongsheng Chen et al.   JOURNAL OF ORGANIC CHEMISTRY

Cleavage of C–C Bonds for the Synthesis of C2-Substituted Quinolines and Indoles by Catalyst-Controlled Tandem Annulation of 2-Vinylanilines and Alkynoates

(2018) Jixiang Ni et al.   ORGANIC LETTERS

Synthesis of 2-(Trifluoromethyl)indoles via Domino Trifluoromethylation/Cyclization of 2-Alkynylanilines

(2018) Yibin Ye et al.   ORGANIC LETTERS

Water-Soluble Hypervalent Iodine(III) Having an I–N Bond. A Reagent for the Synthesis of Indoles

(2018) Hai-Dong Xia et al.   ORGANIC LETTERS

PtCl 4 -catalyzed cyclization of N -acetyl-2-alkynylanilines: A mild and efficient synthesis of N -acetyl-2-substituted indoles

(2018) Nattawadee Chaisan et al.   TETRAHEDRON LETTERS

Aromatase Inhibition by 2-methyl indole hydrazone derivatives evaluated via molecular docking and in vitro activity studies

(2018) Senem Ozcan-Sezer et al.   XENOBIOTICA

Kinase PIM1 promotes prostate cancer cell growth via c-Myc-RPS7-driven ribosomal stress

(2018) Changwen Zhang et al.   CARCINOGENESIS

Pyrrole: An insight into recent pharmacological advances with structure activity relationship

(2018) Shujauddin Ahmad et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Substitution at the indole 3 position yields highly potent indolecombretastatins against human tumor cells

(2018) Raquel Álvarez et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis, Biological Evaluation and Molecular Docking of Novel Indole-Aminoquinazoline Hybrids for Anticancer Properties

(2018) Malose Mphahlele et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Fluorine as a Traceless Directing Group for the Regiodivergent Synthesis of Indoles and Tryptophans

(2018) Anna Andries-Ulmer et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

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

(2018) Hui Cong et al.   MOLECULAR PHARMACEUTICS

Recent developments in topoisomerase targeted cancer chemotherapy

(2018) KirkE. Hevener et al.   Acta Pharmaceutica Sinica B

Prodrugs of the cancer cell selective anti-cancer agent (Z)-2-(1H-indol-3-yl)-3-(isoquinolin-5-yl)acrylonitrile (A131) are orally efficacious in a mouse model of resistant colon cancer

(2018) Cheng Shang See et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

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

1,1-Diheterocyclic Ethylenes Derived from Quinaldine and Carbazole as New Tubulin-Polymerization Inhibitors: Synthesis, Metabolism, and Biological Evaluation

(2018) Timothée Naret et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis of Functionalized Indoles via Palladium-Catalyzed Aerobic Cycloisomerization of o-Allylanilines Using Organic Redox Cocatalyst

(2018) Xiao-Shan Ning et al.   JOURNAL OF ORGANIC CHEMISTRY

Novel anti-cancer agents: design, synthesis, biological activity, molecular docking, and MD simulations of 2, 3, 4, 5-tetrahydro-1H-pyrido-[4,3-b]indole derivatives

(2018) Yu Feng et al.   MEDICINAL CHEMISTRY RESEARCH

Synthesis of Indoles via Electron-Catalyzed Intramolecular C–N Bond Formation

(2018) Dmitry I. Bugaenko et al.   ORGANIC LETTERS

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

Design, synthesis and biological evaluation of novel indole derivatives as potential HDAC/BRD4 dual inhibitors and anti-leukemia agents

(2018) Gaoliang Cheng et al.   BIOORGANIC 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

Bio-guided search of active indole alkaloids from Tabernaemontana catharinensis: Antitumour activity, toxicity in silico and molecular modelling studies

(2018) Pauline Fagundes Rosales et al.   BIOORGANIC 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

Design, synthesis and anticancer properties of Iso CombretaQuinolines as potent tubulin assembly inhibitors

(2017) Ilhem Khelifi et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Structure-activity relationship (SAR) study and design strategies of nitrogen-containing heterocyclic moieties for their anticancer activities

(2017) Jawaid Akhtar et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Thiosemicarbazones and 4-thiazolidinones indole-based derivatives: Synthesis, evaluation of antiproliferative activity, cell death mechanisms and topoisomerase inhibition assay

(2017) Jamerson Ferreira de Oliveira et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Artemisinin as an anticancer drug: Recent advances in target profiling and mechanisms of action

(2017) Yin Kwan Wong et al.   MEDICINAL RESEARCH REVIEWS

Recent advances in combretastatin based derivatives and prodrugs as antimitotic agents

(2017) Zaki S. Seddigi et al.   MedChemComm

Recent Advances in Heterocyclic Tubulin Inhibitors Targeting the Colchicine Binding Site

(2016) Xiaoxin Wu et al.   Anti-Cancer Agents in Medicinal Chemistry

Synthesis and cytotoxic activity of novel hexahydropyrrolo[2,3- b ]indole imidazolium salts

(2016) Yunjing Zhou et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

A general synthesis of arylindoles and (1-arylvinyl)carbazoles via a one-pot reaction from N-tosylhydrazones and 2-nitro-haloarenes and their potential application to colon cancer

(2016) Tourin Bzeih et al.   CHEMICAL COMMUNICATIONS

Pyrrole: An emerging scaffold for construction of valuable therapeutic agents

(2016) Somnath S. Gholap   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and preliminary evaluation of 3-thiocyanato-1H-indoles as potential anticancer agents

(2016) Margiani P. Fortes et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Indole molecules as inhibitors of tubulin polymerization: potential new anticancer agents, an update (2013–2015)

(2016) Renukadevi Patil et al.   Future Medicinal Chemistry

Blocking Blood Flow to Solid Tumors by Destabilizing Tubulin: An Approach to Targeting Tumor Growth

(2016) María-Jesús Pérez-Pérez et al.   JOURNAL OF MEDICINAL CHEMISTRY

Benzo[b]tryptanthrin Inhibits MDR1, Topoisomerase Activity, and Reverses Adriamycin Resistance in Breast Cancer Cells

(2015) Kyu-Yeon Jun et al.   ChemMedChem

Heterocyclic Scaffolds: Centrality in Anticancer Drug Development

(2015) Imran Ali et al.   CURRENT DRUG TARGETS

Design, synthesis and antiproliferative activity of novel heterobivalent hybrids based on imidazo[2,1- b ][1,3,4]thiadiazole and imidazo[2,1- b ][1,3]thiazole scaffolds

(2015) Romeo Romagnoli et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

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 and identification of α-cyano bis(indolyl)chalcones as novel anticancer agents

(2014) Dalip Kumar et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

An Overview on 2-arylquinolin-4(1H)-ones and Related Structures as Tubulin Polymerisation Inhibitors

(2014) Davide Carta et al.   CURRENT TOPICS IN MEDICINAL CHEMISTRY

Recent developments of metal N-heterocyclic carbenes as anticancer agents

(2014) Sainath Babaji Aher et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals

(2014) Edon Vitaku et al.   JOURNAL OF MEDICINAL CHEMISTRY

Synthesis and pharmacological evaluation of novel bisindolylalkanes analogues

(2013) Ya-Li Song et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Artemisinin-Polypyrrole Conjugates: Synthesis, DNA Binding Studies and Preliminary Antiproliferative Evaluation

(2013) Louise La Pensée et al.   ChemMedChem

Drugging Topoisomerases: Lessons and Challenges

(2012) Yves Pommier   ACS Chemical Biology

Design and Synthesis of Some Novel 2,3,4,5-Tetrahydro-1H-pyrido[4,3-b]indoles as Potential c-Met Inhibitors

(2012) Lianbao Ye et al.   HELVETICA CHIMICA ACTA

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

(2012) Yan Lu et al.   PHARMACEUTICAL RESEARCH

Combretastatin-like chalcones as inhibitors of microtubule polymerization. Part 1: Synthesis and biological evaluation of antivascular activity

(2009) Sylvie Ducki et al.   BIOORGANIC & 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

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

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