Cis,cis,trans-[PtIVCl2(NH3)2(perillato)2], a dual-action prodrug with excellent cytotoxic and antimetastatic activity

Two Pt(iv) conjugates containing one or two molecules of perillic acid (4-isopropenylcyclohexene-1-carboxylic acid), an active metabolite of limonene, were synthesized both with traditional and microwave-assisted methods and characterized. Their antiproliferative activity was tested on a panel of human tumor cell lines. In particular, cis,cis,trans-[(PtCl2)-Cl-IV(NH3)(2)(perillato)(2)] exhibited excellent antiproliferative and antimetastatic activity on A-549 lung tumor cells at nanomolar concentrations. A number of in vitro biological tests were performed to decipher some aspects of its mechanism of action, including transwell migration and invasion as well as wound healing assay.

Automated summary

Two Pt(iv) conjugates containing perillic acid were successfully synthesized, with one showing excellent antiproliferative and antimetastatic activity on lung tumor cells, and various in vitro biological tests were conducted to decipher some aspects of its mechanism of action.