Article Sidebar

PDF
Date Published: 12/06/2022
Online Published: 12/06/2023
Abstract Views: 452
Views PDF: 316
Issue
No. 46 (2022)
Section
Article
How to Cite
Cao, T. C. N., & La, B. N. (2023). SYNTHESIS AND CYTOTOXIC ACTIVITY EVALUATION OF BENZIMIDAZOLE DERIVATIVES. Cantho Journal of Medicine and Pharmacy, 46, 55-62. https://tapchi.ctump.edu.vn/index.php/ctump/article/view/907

SYNTHESIS AND CYTOTOXIC ACTIVITY EVALUATION OF BENZIMIDAZOLE DERIVATIVES

Thi Cam Nhung Cao1,, Bao Ngoc La1
1 Hue University of Medicine and Pharmacy

Main Article Content

Abstract

Background: Presently, many scientists are interested in synthesis and screening of biological activity towards anti-cancer effects of new compounds. In order to create a basis for the development of new highly active cancer drugs, we selected the synthesis of new derivatives from the benzimidazole framework and tested their cytotoxic activity. Objectives: The main objective was to synthesize some benzimidazole derivatives and test their cytotoxicity on human cancer cell lines. Material and Methods: A series of benzimidazole derivatives were synthesized by the condensation of ethyl 1H-benzimidazole-2-carboxylate or 2- hydrazinobenzimidazole with substituted aromatic aldehydes. Their structural identification was based on 2D-NMR and MS data. The in vitro cytotoxic activities of all synthesized compounds against human lung carcinoma cells (A549), human breast carcinoma cells (MCF7) and human cervical carcinoma cells (Hela) were evaluated by the SRB assay. Results: Four compounds of benzimidazole were synthesized and determined their structures including: 4-methoxybenzylidene-1H-benzimidazole-2-carbohydrazide (2a),     4-chlorobenzylidene-1H-benzimidazole-2-carbohydrazide    (2b),     2-(2-(4- chlorobenzylidene)hydrazinyl)-1H-benzimidazole  (2c),     2-(2-(4-nitrobenzylidene)hydrazinyl)-1H- benzimidazole (2d). The result showed that compounds 2b and 2d exhibited activity against the tested cell lines with IC50 values ranging from 63,42 to 90,28 µg/mL. Conclusion: In this study, benzimidazole derivatives were synthesized and evaluated for their cytotoxic activity.

Article Details

Keywords

benzimidazole derivatives, synthesis, cytotoxic activity

References

1. Alley MC, Scudiero DA, Monks A, Hursey ML, Czerwinski MJ, Fine DL, Abbott BJ, Mayo JG, Shoemaker RH, Boyd MR (1988), Feasibility of drug screening with panels of human tumor cell lines using a microculture tetrazolium assay, Cancer research, vol 48 (3), pp. 589-601.
2. Indira. M. Madawali , Gaviraj E. N, Navanath. V. Kalyane and B. Shivakumar (2019), A Review On Substituted Benzimidazoles: Biologically Active Compounds, Am. J. PharmTech Res., vol 9(03).
3. Renate Determann, Jan Dreher, Knut Baumann, Lutz Preu, Peter G Jones, Frank Totzke, Christoph Schächtele, Michael H G Kubbutat, Conrad Kunick (2012), 2-Anilino-4- (benzimidazol-2-yl) pyrimidines – A multikinase inhibitor scaffold with antiproliferative activity toward cancer cell lines, European journal of medicinal chemistry, vol 53, pp. 254-263.
4. Srinivas Bethi, Matta Vidyasagar, Rajamanohar.K, Venkateshwar Rao J and Sandeep, Gummudavelly (2011), Synthesis and pharmacological evaluation of new benzimidazole derivatives, Der Chemica Sinica, vol 2 (1), pp. 84-90.
5. Valentina Onnis, Monica Demurtas, Alessandro Deplano, Gianfranco Balboni, Anna Baldisserotto, Stefano Manfredini, Salvatore Pacifico, Sandra Liekens, Jan Balzarini Design (2016), Synthesis and Evaluation of Antiproliferative Activity of New Benzimidazolehydrazones, Molecules, vol 21(5), pp. 579
6. Yunqi Li, Chunyan Tan, Chunmei Gao, Cunlong Zhang, Xudong Luan, Xiaowu Chen, Hongxia Liu, Yuzong Chen, Yuyang Jiang (2011), Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitors, Bioorganic & medicinal Chemistry Research, vol 19 (15), pp. 4529-4535.