Synthesis, cytotoxicity and antimalarial activities of thiosemicarbazones and their nickel (II) complexes
Document Type
Article
Publication Date
1-1-2020
Abstract
A series of Schiff base metal complexes with the formulations [Ni(L1)2] (4), [Ni(L2)2] (5) and [Ni(L3)2] (6), (where 1 or L1 = fluorene-2-carboxaldehyde thiosemicarbazone, 2 or L2 = fluorene-2-carboxaldehyde-4-methyl-thiosemicarbazone and 3 or L3 = fluorene-2-carboxaldehyde-4-ethyl-thiosemicarbazone) have been synthesised. The compounds were characterised by FT-IR, 1H NMR, 13C NMR, and single crystal X-Ray diffraction. The results suggested that the thiosemicarbazone ligands behaved as bidentate ligands which were coordinated to the Ni(II) ion via their N,S atoms. Among the six compounds tested, two of the nickel complexes which are complexes 5 and 6 exhibited moderate in vitro antimalarial activity with IC50 of 23.79 and 2.29 μM, respectively. It is noteworthy that as the size of the substituent group increases, the antimalarial activity of the compound increases. Complex 6 exhibited the highest antimalarial activity. In addition, ligand 3 and complex 4 showed higher cytotoxic activity against HCT 116 human colorectal carcinoma cell line than cisplatin with IC50 of 0.69 and 3.36 μM, respectively. © 2020 Elsevier B.V.
Keywords
Schiff base, Thiosemicarbazone, Metal complex, Anticancer activity, Antimalarial activity
Divisions
fac_med,CHEMISTRY,InstituteofBiologicalSciences
Funders
University of Malaya Research Grant (grant number RP033A-17AFR),MOHE ( FRGS-FP006-2015A ),MyBrain Scholarship
Publication Title
Journal of Molecular Structure
Volume
1211
Publisher
Elsevier