Issue 9, 2021

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

Abstract

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-[PtIVCl2(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.

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

Supplementary files

Article information

Article type
Paper
Submitted
26 Nov 2020
Accepted
09 Feb 2021
First published
09 Feb 2021

Dalton Trans., 2021,50, 3161-3177

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

M. Ravera, E. Gabano, I. Zanellato, B. Rangone, E. Perin, B. Ferrari, M. G. Bottone and D. Osella, Dalton Trans., 2021, 50, 3161 DOI: 10.1039/D0DT04051G

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