Novel Re(I) Complexes as Potential Selective Theranostic Agents in Cancer Cells and In Vivo in Caenorhabditis elegans Tumoral Strains

A series of rhenium­(I) complexes of the type fac-[Re­(CO)3(N^N)­L]0/+, Re1–Re9, was synthesized, where N^N = benzimidazole-derived bidentate ligand with an ester functionality and L = chloride or pyridine-type ligand. The new compounds demonstrated potent activity toward ovarian A2780 cancer cells....

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Bibliographic Details
Published in:Journal of medicinal chemistry 2024-05, Vol.67 (10), p.7891-7910
Main Authors: Marco, Alicia, Ashoo, Pezhman, Hernández-García, Samanta, Martínez-Rodríguez, Pedro, Cutillas, Natalia, Vollrath, Annette, Jordan, Dustin, Janiak, Christoph, Gandía-Herrero, Fernando, Ruiz, José
Format: Article
Language:English
Subjects:
Animals
Antineoplastic Agents - chemical synthesis
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antineoplastic Agents - therapeutic use
Caenorhabditis elegans - drug effects
Cell Line, Tumor
Cell Proliferation - drug effects
Coordination Complexes - chemical synthesis
Coordination Complexes - chemistry
Coordination Complexes - pharmacology
Coordination Complexes - therapeutic use
Drug Screening Assays, Antitumor
Humans
Reactive Oxygen Species - metabolism
Rhenium - chemistry
Theranostic Nanomedicine
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Summary:A series of rhenium­(I) complexes of the type fac-[Re­(CO)3(N^N)­L]0/+, Re1–Re9, was synthesized, where N^N = benzimidazole-derived bidentate ligand with an ester functionality and L = chloride or pyridine-type ligand. The new compounds demonstrated potent activity toward ovarian A2780 cancer cells. The most active complexes, Re7–Re9, incorporating 4-NMe2py, exhibited remarkable activity in 3D HeLa spheroids. The emission in the red region of Re9, which contains an electron-deficient benzothiazole moiety, allowed its operability as a bioimaging tool for in vitro and in vivo visualization. Re9 effectivity was tested in two different C. elegans tumoral strains, JK1466 and MT2124, to broaden the oncogenic pathways studied. The results showed that Re9 was able to reduce the tumor growth in both strains by increasing the ROS production inside the cells. Moreover, the selectivity of the compound toward cancerous cells was remarkable as it did not affect neither the development nor the progeny of the nematodes.
ISSN:0022-2623
1520-4804
DOI:10.1021/acs.jmedchem.3c01869