Novel hydrophilic cis-bis(cyclopentylamine)platinum(II) complexes: Synthesis, characterization, antitumor activity and interaction with DNA

Abstract

Cisplatin-type derivatives cis-bis(cyclopentylamine)bis(alkoxyacetato- κO)platinum(II) (alkoxyacetate = ethoxyacetate, isopropoxyacetate and tert-butoxyacetate) (1-3) have been synthesized and characterized in this study. Replacement of chloride anions in the precursor cis- dichlorobis(cyclopentylamine)platinum(II) with alkoxyacetate improved the water solubility of resulting complexes. The antiproliferative study by WST-8 assay revealed that all complexes showed higher in vitro antitumor effect than carboplatin against four tumor cell lines. Especially, complex 1 exhibited high in vitro cytotoxicity comparable to cisplatin on HCT116, A549, and SGC7901 cell lines. The agarose gel electrophoresis experiment has also been carried out to investigate the interaction of complex 1 with plasmid DNA, which demonstrated a different DNA unwinding pattern in comparison with cisplatin. © 2012 Elsevier B.V. All rights reserved.