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 Trans
; 52(20): 6934-6944, 2023 May 22.
Article
in En
| MEDLINE
| ID: mdl-36916301
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.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Rhenium
/
Coordination Complexes
/
Heterocyclic Compounds
Limits:
Animals
/
Humans
Language:
En
Journal:
Dalton Trans
Journal subject:
QUIMICA
Year:
2023
Document type:
Article
Affiliation country:
Country of publication: