Gold(III) complexes as a new family of cytotoxic and antitumor agents.
In recent years, owing to the contributions of a few research groups, some new gold(III) compounds--either simple coordination complexes or organogold compounds--have been prepared that are sufficiently stable under physiological conditions and are promising candidates for pharmacological testing as cytotoxic and antitumor agents. In vitro pharmacological studies point out that some of these novel gold(III) complexes are highly cytotoxic toward cultured human tumor cell lines and are able to overcome resistance to platinum. Significant differences in the spectrum of action were observed compared with cisplatin. Studies are in progress to elucidate the mechanism of action of these compounds. The cellular effects of two representative gold(III) complexes are described. Preliminary results on binding to DNA in vitro are presented, pointing out that the interactions are generally weak. The implications of these results for the development of gold(III) complexes as a new family of cytotoxic and antitumor agents are discussed.
Department of Chemistry, University of Florence, Via Gino Capponi 7, 50121, Italy.
Giordana
G
Marcon
Luigi
L
Messori
Pierluigi
P
Orioli
D000970:Antineoplastic Agents / Q000494:pharmacology*; D001665:Binding Sites; D002453:Cell Cycle / Q000187:drug effects; D002945:Cisplatin / Q000494:pharmacology; D020552:Comet Assay; D004247:DNA / Q000737:chemistry / Q000187:drug effects*; D004249:DNA Damage; D019008:Drug Resistance, Neoplasm; D004355:Drug Stability; D006046:Gold / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009690:Nucleic Acid Conformation; D009942:Organometallic Compounds / Q000494:pharmacology; D014407:Tumor Cells, Cultured
D000970:Antineoplastic Agents; D009942:Organometallic Compounds; D006046:Gold; D004247:DNA; C427203:calf thymus DNA; D002945:Cisplatin