[Re(I)(CO)3] complexes with the quinolones oxolinic acid and enrofloxacin (Herx) are prepared.
The rhenium(I) complexes can bind to human or bovine serum albumin proteins.
Intercalation is the most possible binding mode of the Re(I) complexes to DNA.
[Re(CO)3(erx)(imidazole)] presents higher inhibitory topoisomerase IIα activity than free Herx.
Tracer complex [99mTc(CO)3(erx)(im)] can enter K562 cancer cells.