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Gd(iii)–Pt(iv) theranostic contrast agents for tandem MR imaging and chemotherapy

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Abstract

Pt(IV) prodrugs have emerged as versatile therapeutics for addressing issues regarding off-target toxicity and the chemoresistance of classic Pt(II) drugs such as cisplatin and carboplatin. There is significant potential for Pt(IV) complexes to be used as theranostic agents, yet there are currently no reported examples of Gd(III)–Pt(IV) agents for simultaneous MR imaging and chemotherapy. Here we report the synthesis, characterization, and in vitro efficacy of two Gd(III)–Pt(IV) agents, GP1 and GP2. Both agents are water soluble and stable under extracellularly relevant conditions but are reduced under intracellular conditions. Both are cytotoxic in multiple cancer cell lines, cell permeable, and significantly enhance the T1-weighted MR contrast of multiple cell lines. Thus, GP1 and GP2 are promising agents for tandem MR imaging and chemotherapy and provide a versatile platform through which future Gd(III)–Pt(IV) agents can be developed.

Graphical abstract: Gd(iii)–Pt(iv) theranostic contrast agents for tandem MR imaging and chemotherapy

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Supplementary files

Article information


Submitted
22 Nov 2019
Accepted
28 Jan 2020
First published
28 Jan 2020

This article is Open Access
All publication charges for this article have been paid for by the Royal Society of Chemistry

Chem. Sci., 2020, Advance Article
Article type
Edge Article

Gd(III)–Pt(IV) theranostic contrast agents for tandem MR imaging and chemotherapy

C. J. Adams and T. J. Meade, Chem. Sci., 2020, Advance Article , DOI: 10.1039/C9SC05937G

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