Anticancer activity studies of novel metal complexes of ligands derived from polycyclic aromatic compound via greener route

Kumbar, Mahantesh; Patil, Sangamesh A.; Toragalmath, Shivakumar S.; Kinnal, Shivashankar M.; Shettar, Arun; Hosakeri, Joy H.

Methoxy and tert-butyl substituted carboxamide, carboxylic acid and hydrazone Schiff base groups have been assembled into our newly designed fluorenone based ligands and prepared coordination compounds of some first row transition metals and characterized thoroughly with spectroscopic ((1)H and (13)C NMR, IR, GC–MS, UV–Vis), analytical, TGA and molar conductance measurements. The stoichiometry of all the metal complexes is found to be 1: 2 (M: L(2)) with the general formula, [M(L)(2)], where L is a singly deprotonated ligand and the geometry of all the metal complexes is found to be octahedral. Ligands and their metal complexes successfully cleaved the pBR322 plasmid DNA and in case of anticancer activity against MCF–7 (human breast adenocarcinoma) cell line, the synthesized compounds found to exhibit excellent activity with prominent apoptotic effect which is characterized by cell shrinkage, cell breakage and turgidity and results were compared with the standard drug cisplatin. Very significant anticancer activity was observed for compounds L(1)H, Cu(L(1))(2), Cu(L(2))(2), Ni(L(1))(2) and Ni(L(2))(2) with IC(50) value of <10 μgmL(−1). Molecular docking studies were performed to assess the bonding mode of synthesized compounds. In case of antioxidant activity study, the compounds L(1)H, Ni(L(1))(2), Cu(L(1))(2), Cu(L(2))(2) and Ni(L(2))(2) exhibited significant scavenging activity with good percentage when compared with remaining tested compounds.