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Unravelling the anticancer potential of a square planar copper complex: toward non-platinum chemotherapy

Malik, MA and Raza, MK and Mohammed, A and Wani, MY and Al-Bogami, AS and Hashmi, AA (2021) Unravelling the anticancer potential of a square planar copper complex: toward non-platinum chemotherapy. In: RSC Advances, 11 (62). pp. 39349-39361.

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Official URL: https://doi.org/10.1039/d1ra06227a


Coordination compounds from simple transition metals are robust substitutes for platinum-based complexes due to their remarkable anticancer properties. In a quest to find new metal complexes that could substitute or augment the platinum based chemotherapy we synthesized three transition metal complexesC1-C3with Cu(ii), Ni(ii), and Co(ii) as the central metal ions, respectively, and evaluated them for their anticancer activity against the human keratinocyte (HaCaT) cell line and human cervical cancer (HeLa) cell lines. These complexes showed different activity profiles with the square planar copper complexC1being the most active with IC50values lower than those of the widely used anticancer drug cisplatin. Assessment of the morphological changes by DAPI staining and ROS generation by DCFH-DA assay exposed that the cell death occurred by caspase-3 mediated apoptosis.C1displayed interesting interactions with Ct-DNA, evidenced by absorption spectroscopy and validated by docking studies. Together, our results suggest that binding of the ligand to the DNA-binding domain of the p53 tumor suppressor (p53DBD) protein and the induction of the apoptotic hallmark protein, caspase-3, upon treatment with the metal complex could be positively attributed to a higher level of ROS and the subsequent DNA damage (oxidation), generated by the complexC1, that could well explain the interesting anticancer activity observed for this complex. © The Royal Society of Chemistry 2021.

Item Type: Journal Article
Publication: RSC Advances
Publisher: Royal Society of Chemistry
Additional Information: The copyright for this article belongs to the Author.
Keywords: Absorption spectroscopy; Cell culture; Cell death; Chemotherapy; Cobalt compounds; Coordination reactions; Copper compounds; DNA; Lanthanum compounds; Metal ions; Nickel compounds; Palladium compounds; Platinum compounds; Proteins; Synthesis (chemical); Transition metals, Anticancer activities; Anticancer potentials; Anticancer properties; Caspase-3; Cell lines; Coordination compounds; Copper complexes; Non-platinum; Platinum-based chemotherapy; Simple++, Metal complexes
Department/Centre: Division of Chemical Sciences > Inorganic & Physical Chemistry
Date Deposited: 12 Jan 2022 05:46
Last Modified: 12 Jan 2022 05:46
URI: http://eprints.iisc.ac.in/id/eprint/70929

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