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Novel 2-(5-Arylthiophen-2-yl)-benzoazole Cyclometalated Iridium(III) dppz Complexes Exhibit Selective Phototoxicity in Cancer Cells by Lysosomal Damage and Oncosis
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SYSNO ASEP 0582097 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Novel 2-(5-Arylthiophen-2-yl)-benzoazole Cyclometalated Iridium(III) dppz Complexes Exhibit Selective Phototoxicity in Cancer Cells by Lysosomal Damage and Oncosis Author(s) Kašpárková, Jana (BFU-R) RID, ORCID
Hernandez-Garcia, A. (ES)
Kostrhunová, Hana (BFU-R) RID, ORCID
Goicuria, M. (ES)
Novohradský, Vojtěch (BFU-R) ORCID
Bautista, D. (ES)
Marková, Lenka (BFU-R) ORCID
Santana, M.D. (ES)
Brabec, Viktor (BFU-R) RID, ORCID
Ruiz, J. (ES)Number of authors 10 Source Title Journal of Medicinal Chemistry. - : American Chemical Society - ISSN 0022-2623
Roč. 67, č. 1 (2023), s. 691-708Number of pages 18 s. Publication form Print - P Language eng - English Country US - United States Keywords photodynamic anticancer ; carbene complexes ; apoptosis ; therapy ; necrosis Subject RIV FR - Pharmacology ; Medidal Chemistry OECD category Pharmacology and pharmacy R&D Projects GA23-06316S GA ČR - Czech Science Foundation (CSF) Method of publishing Open access Institutional support BFU-R - RVO:68081707 UT WOS 001141743200001 EID SCOPUS 85181575081 DOI 10.1021/acs.jmedchem.3c01978 Annotation A second-generation series of biscyclometalated 2-(5-aryl-thienyl)-benzimidazole andbenzothiazole Ir(III) dppz complexes [Ir(C^N)(2)(dppz)](+), Ir1-Ir4, were rationally designed and synthesized, where the aryl group attached to the thienyl ring was p-CF3C6H4 or p-Me2NC6H4. These new Ir(III) complexes were assessed as photosensitizers to explore the structure-activity correlations for their potential use in biocompatible anticancer photodynamic therapy. When irradiated with blue light, the complexes exhibited high selective potency across several cancer cell lines predisposed to photodynamic therapy, the benzothiazole derivatives (Ir1 and Ir2) were the best performers, Ir2 being also activatable with green or red light. Notably, when irradiated, the complexes induced leakage of lysosomal content into the cytoplasm of HeLa cancer cells and induced oncosis-like cell death. The capability of the new Ir complexes to photoinduce cell death in 3D HeLa spheroids has also been demonstrated. The investigated Ir complexes can also catalytically photo-oxidate NADH and photogenerate O-1(2) and/or (OH)-O-center dot in cell-free media. Workplace Institute of Biophysics Contact Jana Poláková, polakova@ibp.cz, Tel.: 541 517 244 Year of Publishing 2024 Electronic address https://pubs.acs.org/doi/10.1021/acs.jmedchem.3c01978
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