Dinuclear zinc bis(thiosemicarbazone) complexes: Synthesis, in vitro anticancer activity, cellular uptake and DNA interaction study

Palanimuthu, Duraippandi and Samuelson, Ashoka G (2013) Dinuclear zinc bis(thiosemicarbazone) complexes: Synthesis, in vitro anticancer activity, cellular uptake and DNA interaction study. In: INORGANICA CHIMICA ACTA, 408 . pp. 152-161.

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Abstract

Four dinucleating bis(thiosemicarbazone) ligands and their zinc complexes have been synthesized and characterized by multinuclear NMR (H-1 and C-13), IR, UV-Vis, ESI-MS and fluorescence spectroscopic techniques. Their purity was assessed by elemental analysis. Cytotoxicity was tested against five human cancer cell lines using the sulphorhodamine B (SRB) assay, where one of the complexes, 1,3-bis{biacetyl-2'-(4 `'-N-pyrrolidinylthiosemicarbazone)-3'-(4 `'-N-pyrrolidinylthiosemicarbazone) zinc(II)} propane (6), was found to be quite cytotoxic against MCF-7 (breast cancer) and HepG2 (hepatoma cancer) cell lines, with a potency similar to that of the well known anticancer drug adriamycin. It is evident from the cellular uptake studies that the uptake is same for the active complex 6 and the inactive complex 8 (1,6-bis{biacetyl- 2'-(4 `'-N-pyrrolidinylthiosemicarbazone)-3'-(4 `'-N-pyrrolidinylthiosemicarbazone) zinc(II)} hexane) in MCF-7 and HepG2 cell lines. In vitro DNA binding and cleavage studies revealed that all complexes bind with DNA through electrostatic interaction, and cause no significant cleavage of DNA. (C) 2'13 Elsevier B. V. All rights reserved.

Item Type:	Journal Article
Publication:	INORGANICA CHIMICA ACTA
Publisher:	ELSEVIER SCIENCE SA
Additional Information:	copyright for this article belongs to ELSEVIER SCIENCE
Keywords:	Bis(thiosemicarbazone); Zinc; Dinuclear complex; Anticancer activity; DNA binding; Cellular uptake
Department/Centre:	Division of Chemical Sciences > Inorganic & Physical Chemistry
Date Deposited:	11 Nov 2013 05:15
Last Modified:	11 Nov 2013 05:15
URI:	http://eprints.iisc.ac.in/id/eprint/47735

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