PUBLICATION
Synthesis, characterization, and in vivo evaluation of the anticancer activity of a series of 5- and 6-(halomethyl)-2,2'-bipyridine rhenium tricarbonyl complexes
- Authors
- Nasiri Sovari, S., Kolly, I., Schindler, K., Djuric, A., Srdic-Rajic, T., Crochet, A., Pavic, A., Zobi, F.
- ID
- ZDB-PUB-230315-37
- Date
- 2023
- Source
- Dalton transactions (Cambridge, England : 2003) 52(20): 6934-6944 (Journal)
- Registered Authors
- Keywords
- none
- MeSH Terms
-
- Humans
- Ligands
- Zebrafish
- Heterocyclic Compounds*
- Rhenium*
- 2,2'-Dipyridyl
- Coordination Complexes*/pharmacology
- Animals
- PubMed
- 36916301 Full text @ Dalton Trans.
Citation
Nasiri Sovari, S., Kolly, I., Schindler, K., Djuric, A., Srdic-Rajic, T., Crochet, A., Pavic, A., Zobi, F. (2023) Synthesis, characterization, and in vivo evaluation of the anticancer activity of a series of 5- and 6-(halomethyl)-2,2'-bipyridine rhenium tricarbonyl complexes. Dalton transactions (Cambridge, England : 2003). 52(20):6934-6944.
Abstract
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.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping