scholarly journals Synthesis of Some Benzimidazole Derivatives Bearing 1,3,4-Oxadiazole Moiety as Anticancer Agents

2015 ◽  
Keyword(s):  
Anticancer Agents ◽  
Benzimidazole Derivatives

Recent Progress of Benzimidazole Hybrids for Anticancer Potential

2020 ◽  
Vol 27 (35) ◽  
pp. 5970-6014 ◽  
Author(s):  
Md. Jawaid Akhtar ◽  
Mohammad Shahar Yar ◽  
Vinod Kumar Sharma ◽  
Ahsan Ahmed Khan ◽  
Zulphikar Ali ◽  
...  
Keyword(s):  
Anticancer Agents ◽  
Biological Activities ◽  
Alkylating Agents ◽  
American Chemical Society ◽  
Chemical Society ◽  
Benzimidazole Derivatives ◽  
Progressive Development ◽  
Anticancer Properties ◽  
Naturally Occurring ◽  
Nitrogenous Base

This review presents the detailed account of factors leading to cancer and design strategy for the synthesis of benzimidazole derivatives as anticancer agents. The recent survey for cancer treatment in Cancer facts and figures 2017 American Chemical Society has shown progressive development in fighting cancer. Researchers all over the world in both developed and developing countries are in a continuous effort to tackle this serious concern. Benzimidazole and its derivatives showed a broad range of biological activities due to their resemblance with naturally occurring nitrogenous base i.e. purine. The review discussed benzimidazole derivatives showing anticancer properties through a different mechanism viz. intercalation, alkylating agents, topoisomerases, DHFR enzymes, and tubulin inhibitors. Benzimidazole derivatives act through a different mechanism and the substituents reported from the earlier and recent research articles are prerequisites for the synthesis of targeted based benzimidazole derivatives as anticancer agents. The review focuses on an easy comparison of the substituent essential for potency and selectivity through SAR presented in figures. This will further provide a better outlook or fulfills the challenges faced in the development of novel benzimidazole derivatives as anticancer.

Synthesis and evaluation of new benzimidazole derivatives with hydrazone moiety as anticancer agents

2018 ◽  
Vol 43 (2) ◽  
pp. 151-158 ◽  
Author(s):  
Ulviye Acar Çevik ◽  
Begüm Nurpelin Sağlık ◽  
Cankız Mina Ardıç ◽  
Yusuf Özkay ◽  
Özlem Atlı
Keyword(s):  
Cytotoxic Activity ◽  
Anticancer Agents ◽  
Point Of View ◽  
Current Therapy ◽  
Benzimidazole Derivatives ◽  
Anticancer Activities ◽  
New Chemical Entities ◽  
Nih 3T3 ◽  
Mcf 7

Abstract Objectives: Cancer is one of the leading causes of death throughout the world. Current therapy options suffer from the major limitations of side effects and drug resistance. Thus, continuing search for newer and safer anticancer drugs remains critically important. From this point of view, in the present study benzimidazole-hydrazone derivatives were synthesized by aiming at the identification of new chemical entities as potent anticancer agents. Material and methods: A series of 12 new compounds of 4-(5(6)-substituted-1H-benzimidazol-2-yl)-N′thiophen/furan-2-yl-methylene) benzohydrazide derivatives were synthesized. The structures of the obtained compounds were elucidated using by IR, 1H NMR, 13C NMR, mass spectroscopy and elemental analyses. In vitro cytotoxic activity of the compounds against A549, MCF-7 and NIH/3T3 cell lines was evaluated by MTT assay. Results: Among the tested compounds, compound 3e showed higher cytotoxicity against MCF-7 human breast cancer cells when compared with cisplatin. Also, it has lower cytotoxicty against healthy cell line, NIH/3T3. Conclusions: It was determined that compound 3e showed inhibition towards MCF-7. Considering the substituent effect on cytotoxic activity, compound 3e bearing 2-methylthiophene has attracted attention with its higher anticancer activities.

Synthesis and Biological Evaluation of Some 1,2-Disubstituted Benzimidazole Derivatives as New Potential Anticancer Agents

2013 ◽  
Vol 346 (5) ◽  
pp. 403-414 ◽  
Author(s):  
Leyla Yurttaş ◽  
Şeref Demirayak ◽  
Gülşen A. Çiftçi ◽  
Şafak Ulusoylar Yıldırım ◽  
Zafer A. Kaplancıklı
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Synthesis And Biological Evaluation

Benzimidazole Derivatives as Potential Anticancer Agents

2013 ◽  
Vol 13 (3) ◽  
pp. 399-407
Author(s):  
Ahmed A. El Rashedy ◽  
Hassan Y. Aboul-Enein
Keyword(s):  
Anticancer Agents ◽  
Benzimidazole Derivatives

ChemInform Abstract: Synthesis and Biological Evaluation of Some 1,2-Disubstituted Benzimidazole Derivatives as New Potential Anticancer Agents.

ChemInform ◽  
2013 ◽  
Vol 44 (37) ◽  
pp. no-no
Author(s):  
Leyla Yurttas ◽  
Seref Demirayak ◽  
Guelsen A. Ciftci ◽  
Safak Ulusoylar Yildirim ◽  
Zafer A. Kaplancikli
Keyword(s):  
Anticancer Agents ◽  
Biological Evaluation ◽  
Benzimidazole Derivatives ◽  
Synthesis And Biological Evaluation

Synthesis and preliminary evaluation of selected 2-aryl-5(6)-nitro- 1H-benzimidazole derivatives as potential anticancer agents

2011 ◽  
Vol 34 (2) ◽  
pp. 181-189 ◽  
Author(s):  
Aurelio Romero-Castro ◽  
Ismael León-Rivera ◽  
Laura Citlalli Ávila-Rojas ◽  
Gabriel Navarrete-Vázquez ◽  
Alejandro Nieto-Rodríguez
Keyword(s):  
Anticancer Agents ◽  
Benzimidazole Derivatives ◽  
Preliminary Evaluation

Perspectives of Benzimidazole Derivatives as Anticancer Agents in the New Era

2016 ◽  
Vol 16 (11) ◽  
pp. 1403-1425 ◽  
Author(s):  
Snehlata Yadav ◽  
Balasubramanian Narasimhan ◽  
Harmeet kaur
Keyword(s):  
Anticancer Agents ◽  
Benzimidazole Derivatives ◽  
New Era

Design, Synthesis, SAR Study, Antimicrobial and Anticancer Evaluation of Novel 2-Mercaptobenzimidazole Azomethine Derivatives

2020 ◽  
Vol 20 (15) ◽  
pp. 1559-1571 ◽  
Author(s):  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Siong Meng Lim ◽  
Kalavathy Ramasamy ◽  
Vasudevan Mani ◽  
...  
Keyword(s):  
Anticancer Activity ◽  
Anticancer Agents ◽  
Benzimidazole Derivatives ◽  
Dilution Method ◽  
Anticancer Activities ◽  
Design Synthesis ◽  
Standard Drug ◽  
Wide Range ◽  
Sar Study

Background: Various analogues of benzimidazole are found to be biologically and therapeutically potent against several ailments. Benzimidazole when attached with heterocyclic rings has shown wide range of potential activities. So, from the above provided facts, we altered benzimidazole derivatives so that more potent antagonists could be developed. In the search for a new category of antimicrobial and anticancer agents, novel azomethine of 2-mercaptobenzimidazole derived from 3-(2- (1H-benzo[d]imidazol-2-ylthio)acetamido)benzohydrazide were synthesized. Results and Discussion: The synthesized analogues were characterized by FT-IR, 1H/13C-NMR and MS studies as well C, H, N analysis. All synthesized compounds were evaluated for in vitro antibacterial activity against Gram-positive (B. subtilis), Gram-negative (E. coli, P. aeruginosa, K. pneumoniae and S. typhi) strains and in vitro antifungal activity against C. albicans and A. niger strains by serial dilution method, the minimum inhibitory concentration (MIC) described in μM/ml. The in vitro anticancer activity of synthesized compounds was determined against human colorectal carcinoma cell line (HCT- 116) using 5-fluorouracil as standard drug. Conclusion: In general, most of the synthesized derivatives exhibited significant antimicrobial and anticancer activities. Compounds 8, 10, 15, 16, 17, 20 and 22 showed significant antimicrobial activity towards tested bacterial and fungal strains and compound 26 exhibited significant anticancer activity.

scholarly journals Combined Effect of Caspase-Dependent and Caspase-Independent Apoptosis in the Anticancer Activity of Gold Complexes with Phosphine and Benzimidazole Derivatives

2020 ◽  
Vol 14 (1) ◽  
pp. 10
Author(s):  
Lara Rouco ◽  
Ángeles Sánchez-González ◽  
Rebeca Alvariño ◽  
Amparo Alfonso ◽  
Ezequiel M. Vázquez-López ◽  
...  
Keyword(s):  
Cell Death ◽  
Anticancer Activity ◽  
Anticancer Agents ◽  
Neuroblastoma Cells ◽  
Fluorescence Analysis ◽  
Benzimidazole Derivatives ◽  
Human Neuroblastoma ◽  
Gold Compounds ◽  
Pre Treatment ◽  
Standard Techniques

Since the potential anticancer activity of auranofin was discovered, gold compounds have attracted interest with a view to developing anticancer agents that follow cytotoxic mechanisms other than cisplatin. Two benzimidazole gold(I) derivatives containing triphenylphosphine (Au(pben)(PPh3)) (1) or triethylphosphine (Au(pben)(PEt3)) (2) were prepared and characterized by standard techniques. X-ray crystal structures for 1 and 2 were solved. The cytotoxicity of 1 and 2 was tested in human neuroblastoma SH-SY5Y cells. Cells were incubated with compounds for 24 h with concentrations ranging from 10 µM to 1 nM, and the half-maximal inhibitory concentration (IC50) was determined. 1 and 2 showed an IC50 of 2.7 and 1.6 µM, respectively. In order to better understand the type of cell death induced by compounds, neuroblastoma cells were stained with Annexin-FITC and propidium iodide. The fluorescence analysis revealed that compounds were inducing apoptosis; however, pre-treatment with the caspase inhibitor Z-VAD did not reduce cell death. Analysis of compound effects on caspase-3 activity and reactive oxygen species (ROS) production in SH-SY5Y cells revealed an antiproliferative ability mediated through oxidative stress and both caspase-dependent and caspase-independent mechanisms.

Sign in / Sign up

Export Citation Format

Share Document