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Synthesis, cytotoxicity and structure-activity relationships between ester and amide functionalities in novel acridine-based platinum(II) complexes

Authors
Journal
Journal of Inorganic Biochemistry
0162-0134
Publisher
Elsevier
Volume
110
Identifiers
DOI: 10.1016/j.jinorgbio.2012.02.006
Keywords
  • Acridine
  • Platinum(Ii) Complexes
  • Cytotoxicity
  • Structure–Activity Relationship
Disciplines
  • Biology
  • Pharmacology

Abstract

Abstract In order to improve the pharmacological profile of the anticancer drug cisplatin, several new acridine-based tethered (ethane-1,2-diamine)platinum(II) complexes connected by a polymethylene chain were synthetized. Activity-structure relationship between amide or ester functionalities was explored by changing acridine-9-carboxamide into acridine-9-carboxylate chromophore. The in vitro cytotoxicity of these new complexes was assessed in human colic HCT 116, SW480 and HT-29 cancer cell lines. Series of complexes bearing the acridine-9-carboxylate chromophore displayed higher cytotoxic effect than acridine-9-carboxamide complexes, with gradual effect according to the size of the polymethylene linker.

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