Journal
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
Volume 2021, Issue 16, Pages 1551-1564Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejic.202100132
Keywords
Anticancer agents; Density functional calculations; Iridium; Metallodrugs; Phosphorescence
Categories
Funding
- Universite de Strasbourg
- CNRS
- International Centre for Frontier Research in Chemistry (icFRC)
- Labex CSC within the Investissement d'Avenir program [ANR-10-LABX-0026 CSC, ANR-10-IDEX-0002-02]
- French Agence Nationale de Recherche (ANR) [ANR-18-CE06-007-01]
- French Ministere de lEducation Nationale, de la Recherche et de la Technologie
- Idex Interdisciplinaire [CF/PN/CB/No2017-973-5]
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A novel family of Ir-III complexes containing a pyridoannelated N-heterocyclic carbene has been synthesized and characterized, showing rare dual emission behavior. These compounds exhibit significantly higher anticancer activity in vitro compared to a market drug, with one compound demonstrating powerful mitochondrial dysfunctioning activity and efficient reactive oxygen species production leading to cell death through apoptosis.
A novel family of Ir-III complexes bearing a pyridoannelated N-heterocyclic carbene is herein described. The target compounds 1-5 are straightforwardly prepared and fully characterized. Comprehensive investigation of their optical properties reveals a rare case of dual emission ascribed to two excited states localized onto different portions of the molecule, as confirmed by both optical spectroscopy and time-dependent density functional calculations including spin-orbit coupling. The cytotoxicity against cancer cell lines is investigated as well. Remarkably, 2-5 show up to 50-fold higher anticancer activity in vitro compared to oxaliplatin market drug with concentration values required to reduce by 50 % the cell viability (IC50) in the low mu M range. Finally, in-depth biological investigation on the most cytotoxic compound 4 reveals its powerful mitochondrial dysfunctioning activity and efficient reactive oxygen species production, associated with apoptosis as the mechanism of cell death.
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