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Systematic investigation of the antiproliferative activity of a series of ruthenium terpyridine complexes


Karges, Johannes; Blacque, Olivier; Jakubaszek, Marta; Goud, Bruno; Goldner, Philippe; Gasser, Gilles (2019). Systematic investigation of the antiproliferative activity of a series of ruthenium terpyridine complexes. Journal of Inorganic Biochemistry, 198:110752.

Abstract

Due to acquired resistance or limitations of the currently approved drugs against cancer, there is an urgent need for the development of new classes of compounds. Among others, there is an increasing attention towards the use of Ru(II) polypyridyl complexes. Most studies in the literature were made on complexes based on the coordination of N-donating bidentate ligands to the ruthenium core whereas studies on 2,2':6', 2 ''-terpyridine (terpy) coordinating ligands are relatively scare. However, several studies have shown that Ru(terpy)2 derivatives are able bind to DNA through various binding modes making these compounds potentially suitable as chemotherapeutic agents. Additionally, light irradiation of these compounds was shown to enable DNA cleavage, highlighting their potential use as photosensitizers (PSs) for photodynamic therapy (PDT). In this work, we present the systematic investigation of the potential of 7 complexes of the type Ru(terpy)(terpy-X) (X = H (1), Cl (2), Br (3), OMe (4), COOH (5), COOMe (6), NMe2 (7)) as potential chemotherapeutic agents and PDT PSs. Importantly, six of the seven complexes were found to be stable in human plasma as well as photostable in acetonitrile upon continuous light irradiation (480 nm). The determination of the distribution coefficient logP values for the 7 complexes revealed their good water solubility. Complex 7 was found to be cytotoxic in the micromolar range in the dark as well as to have some phototoxicity upon light exposure at 480 nm in noncancerous retinal pigment epithelium (RPE-1) and cancerous human cervical carcinoma (HeLa) cells.Synopsis: The systematic investigation of the potential of 7 complexes of the type Ru(terpy)(terpy-X) (terpy: 2,2':6', 2 ''-terpyridine; X = H (1), Cl (2), Br (3), OMe (4), COOH (5), COOMe (6), NMe2 (7)) as potential chemotherapeutic agents and photosensitizers for photodynamic therapy is presented.

Abstract

Due to acquired resistance or limitations of the currently approved drugs against cancer, there is an urgent need for the development of new classes of compounds. Among others, there is an increasing attention towards the use of Ru(II) polypyridyl complexes. Most studies in the literature were made on complexes based on the coordination of N-donating bidentate ligands to the ruthenium core whereas studies on 2,2':6', 2 ''-terpyridine (terpy) coordinating ligands are relatively scare. However, several studies have shown that Ru(terpy)2 derivatives are able bind to DNA through various binding modes making these compounds potentially suitable as chemotherapeutic agents. Additionally, light irradiation of these compounds was shown to enable DNA cleavage, highlighting their potential use as photosensitizers (PSs) for photodynamic therapy (PDT). In this work, we present the systematic investigation of the potential of 7 complexes of the type Ru(terpy)(terpy-X) (X = H (1), Cl (2), Br (3), OMe (4), COOH (5), COOMe (6), NMe2 (7)) as potential chemotherapeutic agents and PDT PSs. Importantly, six of the seven complexes were found to be stable in human plasma as well as photostable in acetonitrile upon continuous light irradiation (480 nm). The determination of the distribution coefficient logP values for the 7 complexes revealed their good water solubility. Complex 7 was found to be cytotoxic in the micromolar range in the dark as well as to have some phototoxicity upon light exposure at 480 nm in noncancerous retinal pigment epithelium (RPE-1) and cancerous human cervical carcinoma (HeLa) cells.Synopsis: The systematic investigation of the potential of 7 complexes of the type Ru(terpy)(terpy-X) (terpy: 2,2':6', 2 ''-terpyridine; X = H (1), Cl (2), Br (3), OMe (4), COOH (5), COOMe (6), NMe2 (7)) as potential chemotherapeutic agents and photosensitizers for photodynamic therapy is presented.

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Additional indexing

Item Type:Journal Article, refereed, original work
Communities & Collections:07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Language:English
Date:1 September 2019
Deposited On:07 Feb 2020 08:40
Last Modified:07 Feb 2020 08:40
Publisher:Elsevier
ISSN:0162-0134
OA Status:Closed
Publisher DOI:https://doi.org/10.1016/j.jinorgbio.2019.110752

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