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
- Nasiri Sovari, Sara University of Fribourg
- Kolly, Isabelle University of Fribourg
- Schindler, Kevin ORCID University of Fribourg
- Djuric, Ana Institute for Oncology and Radiology of Serbia, Belgrade, Serbia
- Srdic-Rajic, Tatjana Institute for Oncology and Radiology of Serbia, Belgrade, Serbia
- Crochet, Aurélien ORCID University of Fribourg
- Pavic, Aleksandar University of Belgrade, Serbia
- Zobi, Fabio ORCID University of Fribourg
- 2023
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.
- Faculty
- Faculté des sciences et de médecine
- Department
- Département de Chimie
- Language
-
- English
- Classification
- Chemistry
- License
- CC BY-NC
- Open access status
- hybrid
- Identifiers
-
- DOI 10.1039/D2DT04041G
- ISSN 1477-9226
- ISSN 1477-9234
- Persistent URL
- https://folia.unifr.ch/unifr/documents/330406
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