The discovery of cisplatin and its later approved derivatives started a new era in the bioinorganic medicinal chemistry field but the persistence of severe side-effects along with the emerging of drug resistance evoke the need of a new generation of transition metal-based chemotherapeutics with the aim to overcome these limitations. Given that many transition metal complexes also display interesting photophysical properties, an increasing interest has recently arisen in the development of platinum based theranostic agents, i.e. compounds combining both therapeutic and detection properties in a single entity.1,2 Our research group has synthesised and evaluated for the treatment of triple-negative breast cancer (TNBC) a series of cyclometalated anionic platinum complexes carrying tetrabromocatechol or alizarine as O^O chelating ligands.3 All these complexes resulted emissive in solution and the fluorescence confocal analysis showed their localization in the cytosol of MDA-MB231 cells proving their ability to serve as luminescent probes. By matching these diagnostic imaging properties with the potent cytotoxicity exhibited by the dichloro platinum(II) complex based on 8-aminoquinoline (4.5±µM) and its 5,6,7,8- tetrahydro derivatives on the highly aggressive TNBC cell line,4 a novel series of promising theranostic agents can be developed.

Cytotoxic platinum(II) complexes bearing N-heterocycle rings as novel theranostic agents / I.S. Rimoldi, G. Facchetti, N. Ferri, A. Ionescu, R. Caligiuri, N. Godbert, L. Ricciardi, M. La Deda, M. Ghedini, M. Giovanna Lupo, I. Aiello. ((Intervento presentato al 19. convegno BIOMET 2020-XIX Workshop on Pharmacobiometallics tenutosi a Ancona nel 2020.

Cytotoxic platinum(II) complexes bearing N-heterocycle rings as novel theranostic agents

I.S. Rimoldi
Primo
;
G. Facchetti
Secondo
;
N. Ferri;
2020

Abstract

The discovery of cisplatin and its later approved derivatives started a new era in the bioinorganic medicinal chemistry field but the persistence of severe side-effects along with the emerging of drug resistance evoke the need of a new generation of transition metal-based chemotherapeutics with the aim to overcome these limitations. Given that many transition metal complexes also display interesting photophysical properties, an increasing interest has recently arisen in the development of platinum based theranostic agents, i.e. compounds combining both therapeutic and detection properties in a single entity.1,2 Our research group has synthesised and evaluated for the treatment of triple-negative breast cancer (TNBC) a series of cyclometalated anionic platinum complexes carrying tetrabromocatechol or alizarine as O^O chelating ligands.3 All these complexes resulted emissive in solution and the fluorescence confocal analysis showed their localization in the cytosol of MDA-MB231 cells proving their ability to serve as luminescent probes. By matching these diagnostic imaging properties with the potent cytotoxicity exhibited by the dichloro platinum(II) complex based on 8-aminoquinoline (4.5±µM) and its 5,6,7,8- tetrahydro derivatives on the highly aggressive TNBC cell line,4 a novel series of promising theranostic agents can be developed.
feb-2020
Settore CHIM/03 - Chimica Generale e Inorganica
Settore BIO/14 - Farmacologia
Consorzio interuniversitario di ricerca in chimica dei metalli nei sistemi biologici
Dipartimento di Scienze della Vita e dell'Ambiente Università politecnica delle Marche
https://www.biomet2020.it/wp-content/uploads/2020/03/Libro-degli-Abstracts-Biomet-2020.pdf
Cytotoxic platinum(II) complexes bearing N-heterocycle rings as novel theranostic agents / I.S. Rimoldi, G. Facchetti, N. Ferri, A. Ionescu, R. Caligiuri, N. Godbert, L. Ricciardi, M. La Deda, M. Ghedini, M. Giovanna Lupo, I. Aiello. ((Intervento presentato al 19. convegno BIOMET 2020-XIX Workshop on Pharmacobiometallics tenutosi a Ancona nel 2020.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/717675
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