Journal article
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Synthesis, characterization, and in vivo evaluation of the anticancer activity of a series of 5- and 6-(halomethyl)-2,2′-bipyridine rhenium tricarbonyl complexes
DOKPE
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Nasiri Sovari, Sara
University of Fribourg
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Kolly, Isabelle
University of Fribourg
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Schindler, Kevin
ORCID
University of Fribourg
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Djuric, Ana
Institute for Oncology and Radiology of Serbia, Belgrade, Serbia
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Srdic-Rajic, Tatjana
Institute for Oncology and Radiology of Serbia, Belgrade, Serbia
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Crochet, Aurélien
ORCID
University of Fribourg
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Pavic, Aleksandar
University of Belgrade, Serbia
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Zobi, Fabio
ORCID
University of Fribourg
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Published in:
- Dalton Transactions. - London, UK: Royal Society of Chemistry (RSC). - 2023, vol. 52, no. 20, p. 6934-6944
English
We report the synthesis, characterization, and in vivo evaluation of the anticancer activity of a series of 5- and 6-(halomethyl)-2,2′-bipyridine rhenium tricarbonyl complexes. The study was promoted in order to understand if the presence and position of a reactive halomethyl substituent on the diimine ligand system of fac-[Re(CO)3]+ species may be a key molecular feature for the design of active and non-toxic anticancer agents. Only compounds potentially able to undergo ligand-based alkylating reactions show significant antiproliferative activity against colorectal and pancreatic cell lines. Of the new species presented in this study, one compound (5-(chloromethyl)-2,2′-bipyridine derivative) shows significant inhibition of pancreatic tumour growth in vivo in zebrafish-Panc-1 xenografts. The complex is noticeably effective at 8 μM concentration, lower than its in vitro IC50 values, being also capable of inhibiting in vivo cancer cells dissemination.
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Faculty
- Faculté des sciences et de médecine
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Department
- Département de Chimie
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Language
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Classification
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Chemistry
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License
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CC BY-NC
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Open access status
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hybrid
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Identifiers
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Persistent URL
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https://folia.unifr.ch/unifr/documents/330406
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