Design, Synthesis and Evaluation of Hybrid 2-Heteroaryl Benzimidazole- Chalcone Derivatives as Anticancer Agents

Author(s): Gajula Shyam Kumar, Bethi Rathnakar, Sridhar Gattu, Surender Singh Jadav, Nimma Rameshwar, Shireesha Boyapati, Mavurapu Satyanarayana*

Journal Name: Letters in Organic Chemistry

Volume 18 , Issue 10 , 2021

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A series of 2-heteroaryl benzimidazole-chalcone hybrids were synthesized and the anticancer activity was estimated by MTT assay in human breast, lung, colon, and ovarian cancer cell lines. The biological results indicate that the compounds showed good anticancer activity with IC50 value in the range of 0.056-19.5 μM. Compound 11b with hexa methoxy groups, bearing three methoxy groups on each terminal aryl ring exhibited a significant IC50 value (56 nM) against human breast carcinoma cells, which is 37 times higher potency in comparison with the reference Etoposide. Further compounds substituted variably with methoxy and nitro groups on the phenyl ring of chalcone showed more promising anticancer activity than the compounds with unsubstituted phenyl ring or variably alkyl-substituted phenyl ring of chalcone. The molecular docking results indicate that the synthesized compounds bind in the active site of Abl tyrosine kinase, the target of anticancer drug Imatinib. The present study provides the synergistic effect of hybrids, benzimidazole-chalcones as potential anticancer agents that will aid in the discovery of new anticancer agents.

Keywords: Chalcones, benzimidazoles, hybrids, anticancer activity, licochalcone A, nocodazole, Abl tyrosine kinase, imatinib.

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Article Details

Year: 2021
Published on: 06 November, 2020
Page: [766 - 776]
Pages: 11
DOI: 10.2174/1570178617999201106140951
Price: $95

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