Anticancer Therapeutic Potential of Benzofuran Scaffolds

Overview

Journal RSC Adv

Publisher Royal Society of Chemistry

Specialty Chemistry

Date 2023 Apr 14

PMID 37056966

Authors

Ashraf A Abbas

Kamal M Dawood

Affiliations

Soon will be listed here.

Abstract

Benzofuran moiety is the main component of many biologically active natural and synthetic heterocycles. These heterocycles have unique therapeutic potentials and are involved in various clinical drugs. The reported results confirmed the extraordinary inhibitory potency of such benzofurans against a panel of human cancer cell lines compared with a wide array of reference anticancer drugs. Several publications about the anticancer potencies of benzofuran-based heterocycles were encountered. The recent developments of anticancer activities of both natural and synthetic benzofuran scaffolds during 2019-2022 are thoroughly covered. Many of the described benzofurans are promising candidates for development as anticancer agents based on their outstanding inhibitory potency against a panel of human cancer cells compared with reference anticancer drugs. These findings encourage medicinal chemists to explore new areas to improve human health and reduce suffering.

Citing Articles

The synthesis and investigation of novel 3-benzoylbenzofurans and pyrazole derivatives for anti-HIV activity.

Khuzwayo S, Selepe M, Meyer D, Gama N RSC Med Chem. 2025; .

PMID: 40060998 PMC: 11883425. DOI: 10.1039/d4md00844h.

Characterization of Volatilized Compounds in Conventional and Organic Vegetable-Source Alternative Meat-Curing Ingredients.

Sheng S, Silva E, Ricke S, Claus J Molecules. 2025; 30(4).

PMID: 40005146 PMC: 11858521. DOI: 10.3390/molecules30040835.

New Benzofuran-Pyrazole-Based Compounds as Promising Antimicrobial Agents: Design, Synthesis, DNA Gyrase B Inhibition, and In Silico Studies.

Abd El-Karim S, Anwar M, Syam Y, Awad H, El-Dein A, El-Ashrey M Pharmaceuticals (Basel). 2025; 17(12.

PMID: 39770506 PMC: 11676098. DOI: 10.3390/ph17121664.

Synthesis of Benzofuran Derivatives via a DMAP-Mediated Tandem Cyclization Reaction Involving -Hydroxy α-Aminosulfones.

Zhu R, Hou X, Du D Molecules. 2024; 29(16).

PMID: 39202804 PMC: 11357171. DOI: 10.3390/molecules29163725.

Inhibition of Clostridioides difficile toxins TcdA and TcdB by the amiodarone derivative dronedarone.

Matylitsky J, Krieg A, Schumacher J, Borho J, Barth H, Papatheodorou P Naunyn Schmiedebergs Arch Pharmacol. 2024; 397(12):9877-9885.

PMID: 38935126 PMC: 11582217. DOI: 10.1007/s00210-024-03248-8.

References

Abdelhafez O, Ahmed E, Abdel Latif N, Arafa R, Abd Elmageed Z, Ali H . Design and molecular modeling of novel P38α MAPK inhibitors targeting breast cancer, synthesized from oxygen heterocyclic natural compounds. Bioorg Med Chem. 2019; 27(7):1308-1319. DOI: 10.1016/j.bmc.2019.02.027. View

Sivaraman A, Kim J, Harmalkar D, Min K, Park J, Choi Y . Synthesis and Cytotoxicity Studies of Bioactive Benzofurans from and Modified Synthesis of Ailanthoidol, Homoegonol, and Egonol. J Nat Prod. 2020; 83(11):3354-3362. DOI: 10.1021/acs.jnatprod.0c00697. View

Ma L, Tang L, Yi Q . Salvianolic Acids: Potential Source of Natural Drugs for the Treatment of Fibrosis Disease and Cancer. Front Pharmacol. 2019; 10:97. PMC: 6391314. DOI: 10.3389/fphar.2019.00097. View

Radadiya A, Shah A . Bioactive benzofuran derivatives: An insight on lead developments, radioligands and advances of the last decade. Eur J Med Chem. 2015; 97:356-76. DOI: 10.1016/j.ejmech.2015.01.021. View

Mokenapelli S, Thalari G, Vadiyaala N, Yerrabelli J, Irlapati V, Gorityala N . Synthesis, cytotoxicity, and molecular docking of substituted 3-(2-methylbenzofuran-3-yl)-5-(phenoxymethyl)-1,2,4-oxadiazoles. Arch Pharm (Weinheim). 2020; 353(6):e2000006. DOI: 10.1002/ardp.202000006. View

Li Y, Bao L, Song B, Han J, Li H, Zhao F . A new benzoquinone and a new benzofuran from the edible mushroom Neolentinus lepideus and their inhibitory activity in NO production inhibition assay. Food Chem. 2013; 141(3):1614-8. DOI: 10.1016/j.foodchem.2013.04.133. View

Gao C, Sun X, Wu Z, Yuan H, Han H, Huang H . A Novel Benzofuran Derivative Moracin N Induces Autophagy and Apoptosis Through ROS Generation in Lung Cancer. Front Pharmacol. 2020; 11:391. PMC: 7235196. DOI: 10.3389/fphar.2020.00391. View

Cuypers H, Selten G, Quint W, Zijlstra M, Maandag E, Boelens W . Murine leukemia virus-induced T-cell lymphomagenesis: integration of proviruses in a distinct chromosomal region. Cell. 1984; 37(1):141-50. DOI: 10.1016/0092-8674(84)90309-x. View

Zhang G, Zhong L, Bligh S, Guo Y, Zhang C, Zhang M . Bi-bicyclic and bi-tricyclic compounds from Dendrobium thyrsiflorum. Phytochemistry. 2005; 66(10):1113-20. DOI: 10.1016/j.phytochem.2005.04.001. View

10.

Woodgett J . Molecular cloning and expression of glycogen synthase kinase-3/factor A. EMBO J. 1990; 9(8):2431-8. PMC: 552268. DOI: 10.1002/j.1460-2075.1990.tb07419.x. View

11.

Naik R, Harmalkar D, Xu X, Jang K, Lee K . Bioactive benzofuran derivatives: moracins A-Z in medicinal chemistry. Eur J Med Chem. 2014; 90:379-93. DOI: 10.1016/j.ejmech.2014.11.047. View

12.

He X, Gao Y, Hui Z, Shen G, Wang S, Xie T . 4-Hydroxy-3-methylbenzofuran-2-carbohydrazones as novel LSD1 inhibitors. Bioorg Med Chem Lett. 2020; 30(10):127109. DOI: 10.1016/j.bmcl.2020.127109. View

13.

Xu X, Yang Y, Mo X, Wei J, Zhang X, You Q . Design, synthesis, and evaluation of benzofuran derivatives as novel anti-pancreatic carcinoma agents via interfering the hypoxia environment by targeting HIF-1α pathway. Eur J Med Chem. 2017; 137:45-62. DOI: 10.1016/j.ejmech.2017.05.042. View

14.

Salome C, Narbonne V, Ribeiro N, Thuaud F, Serova M, de Gramont A . Benzofuran derivatives as a novel class of inhibitors of mTOR signaling. Eur J Med Chem. 2014; 74:41-9. DOI: 10.1016/j.ejmech.2013.12.020. View

15.

Zhang W, Chu J, Cyr A, Yueh H, Brown L, Wang T . Intercepted Retro-Nazarov Reaction: Syntheses of Amidino-Rocaglate Derivatives and Their Biological Evaluation as eIF4A Inhibitors. J Am Chem Soc. 2019; 141(32):12891-12900. PMC: 6693944. DOI: 10.1021/jacs.9b06446. View

16.

Fan X, He H, Li J, Luo G, Zheng Y, Zhou J . Discovery of 4,6-bis(benzyloxy)-3-phenylbenzofuran as a novel Pin1 inhibitor to suppress hepatocellular carcinoma via upregulating microRNA biogenesis. Bioorg Med Chem. 2019; 27(11):2235-2244. DOI: 10.1016/j.bmc.2019.04.028. View

17.

Li Q, Jian X, Chen Z, Chen L, Huo X, Li Z . Synthesis and biological evaluation of benzofuran-based 3,4,5-trimethoxybenzamide derivatives as novel tubulin polymerization inhibitors. Bioorg Chem. 2020; 102:104076. DOI: 10.1016/j.bioorg.2020.104076. View

18.

Garg A, Garg S, Sahu N, Rani S, Gupta U, Yadav A . Heparin appended ADH-anionic polysaccharide nanoparticles for site-specific delivery of usnic acid. Int J Pharm. 2018; 557:238-253. DOI: 10.1016/j.ijpharm.2018.12.049. View

19.

Chand K, Rajeshwari , Hiremathad A, Singh M, Santos M, Keri R . A review on antioxidant potential of bioactive heterocycle benzofuran: Natural and synthetic derivatives. Pharmacol Rep. 2017; 69(2):281-295. DOI: 10.1016/j.pharep.2016.11.007. View

20.

Siddiqui S, Sahayasheela V, Kolluru S, Pandian G, Santhoshkumar T, Dan V . Discovery of 3-(benzofuran-2-ylmethyl)-1H-indole derivatives as potential autophagy inducers in cervical cancer cells. Bioorg Med Chem Lett. 2020; 30(19):127431. DOI: 10.1016/j.bmcl.2020.127431. View