Journal
CHEMISTRY-A EUROPEAN JOURNAL
Volume 26, Issue 26, Pages 5903-5910Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/chem.202001014
Keywords
antiproliferation; apoptosis; dendrimers; dendrons; fluorescent probes; imaging agents
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Funding
- National Natural Science Foundation of China [21911530230, 21773026, 81761148028]
- Sino-French Cai Yuanpei Programme
- FCT-Fundacao para a Ciencia e a Tecnologia
- Portuguese Government funds through the CQM Strategic Project [PEst-OE/ QUI/UI0674/2013]
- ARDITI-Agencia Regional parao Desenvolvimento da Investigacao Tecnologia through Centro de Qumica da Madeira-CQM+ (Madeira 14-20 Program) [M1420-01-0145-FEDER-000005]
- CNRS (France)
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First-in-class Cu-II and Au-III metaled phosphorus dendrons were synthesized and showed significant antiproliferative activity against several aggressive breast cancer cell lines. The data suggest that the cytotoxicity increases with reducing length of the alkyl chains, whereas the replacement of Cu-II with Au-III considerably increases the antiproliferative activity of metaled phosphorus dendrons. Very interestingly, we found that the cell death pathway is related to the nature of the metal complexed by the plain dendrons. Cu-II metaled dendrons showed a potent caspase-independent cell death pathway, whereas Au-III metaled dendrons displayed a caspase-dependent apoptotic pathway. The complexation of plain dendrons with Au-III increased the cellular lethality versus dendrons with Cu-II and promoted the translocation of Bax into the mitochondria and the release of Cytochrome C (Cyto C).
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