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Molecules 2018, 23(5), 1232; https://doi.org/10.3390/molecules23051232

Evaluation of Transition Metal Complexes of Benzimidazole-Derived Scaffold as Promising Anticancer Chemotherapeutics

1
Department of Pharmacognosy, College of Pharmacy, King Saud University, P.O. Box 2457, 11451 Riyadh, Saudi Arabia
2
Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, 11451 Riyadh, Saudi Arabia
3
Department of Chemistry, College of Science, King Saud University, P.O. Box 2455, 11451 Riyadh, Saudi Arabia
*
Author to whom correspondence should be addressed.
Received: 20 March 2018 / Revised: 8 May 2018 / Accepted: 15 May 2018 / Published: 21 May 2018
(This article belongs to the Section Inorganic Chemistry)
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Abstract

Three new transition metal complexes, Cu(II) 1, Co(II) 2, and Zn(II) 3 with ligand “bimnap” derived from 1-methyl-2-aminobenzimidazole and 2-hydroxynapthaldehyde were synthesized and characterized. The structure of the ligand was determined by single X-ray crystallography. All the three complexes, 13, were examined for the mode of interaction with biomolecule viz., calf thymus-DNA (CT-DNA) using various spectroscopic methods. The nuclease activity was performed against pBR322 DNA that exhibited concentration-dependent degradation of the nucleic acid. The mechanism of DNA cleavage was studied by the electrophoretic pattern in the presence of the radical scavengers. Also, the complexes 13 were analyzed for groove binding affinity. Moreover, in vitro cytotoxicities of the complexes 13 were tested against the five human cancer cell lines, i.e., HeLa, SK-MEL-1, HepG2, HT108, and MDA-MB 231. Also, the cell adhesion and migration properties upon treatment of cell lines with complexes 13, and consequently, their cell death pathway via apoptosis and necrosis were analyzed. Further, complexes 13 were studied in vivo for their toxicities and tolerabilities in mice. In sum, the complexes 13 showed merits of an effective anticancer agent in cell lines–based study while minor side effects were observed in vivo. View Full-Text
Keywords: metal complexes; DNA binding/cleavage; cytotoxicity; cell migration/adhesion; apoptosis; toxicity profile metal complexes; DNA binding/cleavage; cytotoxicity; cell migration/adhesion; apoptosis; toxicity profile
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Hussain, A.; AlAjmi, M.F.; Rehman, M.T.; Khan, A.A.; Shaikh, P.A.; Khan, R.A. Evaluation of Transition Metal Complexes of Benzimidazole-Derived Scaffold as Promising Anticancer Chemotherapeutics. Molecules 2018, 23, 1232.

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