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

[ Vol. 18 , Issue. 10 ]

Author(s):

Gajula Shyam Kumar, Bethi Rathnakar, Sridhar Gattu, Surender Singh Jadav, Nimma Rameshwar, Shireesha Boyapati and Mavurapu Satyanarayana*   Pages 766 - 776 ( 11 )

Abstract:


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.

Affiliation:

Department of Pharmaceutical Chemistry, Telangana University, Dichpally, Nizamabad-503322, Department of Pharmaceutical Chemistry, Telangana University, Dichpally, Nizamabad-503322, Organic and Bio-Molecular Division, CSIR-IICT, Tarnaka, Hyderabad-50007, CMCR, Vishnu Institute of Pharmaceutical Education and Research, Narsapur, Medak-502313, Department of Pharmaceutical Chemistry, Telangana University, Dichpally, Nizamabad-503322, Department of Pharmaceutical Chemistry, Telangana University, Dichpally, Nizamabad-503322, Department of Pharmaceutical Chemistry, Telangana University, Dichpally, Nizamabad-503322



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