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Applicant:
Central University of Tamil Nadu 
Author:
Sambantham Karpagam, Radhakrishnan Kartikeyan, Pappaiyan Paravai Nachiyar, MarappanVelusamy, Mani Kannan, Muthukalingam Krishnan, Upendra Chitgupi, Jonathan F. Lovell, Mohammad Abdulkader Akbarsha and Venugopal Rajendiran 
Corresponding Authors:
Venugopal Rajendiran 
DOI #:
doi.org/10.1080/00958972.2019.1680834 
Title:
ROS-mediated cell death induced by mixed ligand copper(II) complexes of L-proline and diimine: effect of co-ligand 
Journal:
JOURNAL OF COORDINATION CHEMISTRY 
Year:
2019 
Volume:
72 
Page:
3102–3127 
Keywords:
Copper complexes; DNA binding and cleavage; protein cleavage; gel electrophoresis; cytotoxicity; ROS 
Abstract:
A series of mixed ligand Cu(II) complexes of the type i) [Cu(L-pro)(diimine)(H2O)n]ClO4 (n = 0 or 1), where L-pro is L-proline and diimine is 2,2′-bipyridine (bpy; 1), ii) 4,4′-dimethyl-2,2′-bipyridine (dmbpy; 2), iii) 1,10-phenanthroline (phen; 3), iv) 5,6-dimethyl-1,10-phenanthroline (5,6-dmp; 4), v) 3,4,7,8-tetramethyl-1,10-phenanthroline (3,4,7,8-tmp; 5), vi) dipyrido-[3,2-f:2′,3′-h]-quinoxaline (dpq; 6) and vii) dipyrido[3,2-a:2′,3′-c]phenazine (dppz; 7) have been synthesized and characterized systematically. The complexes 2 and 3 have been structurally characterized. DNA and protein-binding and cleavage studies revealed that the complex 7 possesses stronger DNA and protein binding efficiency, and also exhibits self-activating DNA cleavage in the absence of an activating agent. The hydrophobic complexes 4 and 5 induced self-activated protein cleavage and yielded a single cleaved fragment each. The cytotoxic property of all the seven complexes was examined by incubation with the human small cell lung carcinoma cell line A549. The complexes 4 and 6 exhibited almost similar cytotoxic properties (IC50=1.4 µM (4) and 1.3 µM (6), which was 9.3 and 10 times, respectively, more efficient than cisplatin (IC50 = 13µM). The complex 4 induced generation of the highest level of intracellular ROS which correlates with its efficient cytotoxic activity and provides scope for further investigation as a potential anticancer agent. 
Entered by:
Rajendiran Venugopal on 2020-08-24 
 
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