Cytotoxicity modulation of ruthenium(II) tris-bathophenanthroline complexes with systematically varied charge

摘要: Abstract A series of four ruthenium(II) complexes Ru(bp)n(bps)3-n (n = 0-3; bp = 4,7-diphenyl-1,10-phenanthroline or bathophenanthroline; and bps = disulfonated 4,7-diphenyl-1,10-phenanthroline bathophenanthroline disulfonate) bearing different charges were synthesized characterized. In aqueous media, all displayed similar photophysical properties which makes this ideal to study the effect charge on cytotoxicity Ru(II) complexes. Ru(bp)32+ (1) Ru(bps)34− (4) are known photosensitizers that penetrate cancer cells possess a significant light-induced cytotoxicity. The newly conceived neutral Ru(bp)2(bps)0 (2) dianionic Ru(bp)(bps)22− (3) also found have uptake as well light-activation properties. Importantly, in dark was successfully tuned upon systematic modulation cationic complex 1 potent against 5 out 6 cell lines tested (MDA-MB-231, MCF-7, B16, SF ML2) highest among with IC50 values 4.0, 3.6, 1.7, 1.0 2.9 μM, respectively. two anionic complexes, 3 4, respective overall −2 −4, not any (IC50 > 200 μM), whereas molecule, 2, (B16, exhibited an intermediate activity 12.8, 3.0 10.3 μM, All presented phototoxicity when activated at 6 h post-incubation, is consistent their fast ability produce singlet oxygen. localization 1–4 within be dependent photoexcitation conditions. charge-activity relationship elucidated work facilitates development new sensitizers for photodynamic therapy.