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

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.

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Synthesis and preliminary evaluation activity studies of novel 4-(aryl/heteroaryl-2-ylmethyl)-6-phenyl-2-[3-(4-substituted-piperazine-1-yl)propyl]pyridazin-3(2H)-one derivatives as anticancer agents

Medicinal Chemistry Research ◽

10.1007/s00044-011-9851-6 ◽

2011 ◽

Vol 21 (10) ◽

pp. 3161-3169 ◽

Cited By ~ 10

Author(s):

M. S. R. Murty ◽

B. Ramalingeswara Rao ◽

Kesur R. Ram ◽

J. S. Yadav ◽

Jayesh Antony ◽

...

Keyword(s):

Anticancer Agents ◽

Preliminary Evaluation ◽

Evaluation Activity ◽

Substituted Piperazine

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

Turkish Journal of Biochemistry ◽

10.1515/tjb-2017-0167 ◽

2018 ◽

Vol 43 (2) ◽

pp. 151-158 ◽

Cited By ~ 3

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.

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