Table 2. Phototoxicity of the PtIV complexes trans,trans,trans-[Pt(N3)2(OH)2(L1)(L2)] following irradiation with blue light (420 nm, 5 J cm–2, TL03, filtered <400 nm).Values are in μM.
Complex | L1 | L2 | A2780 |
A2780cis |
OE19 |
||||||
IC50 | 95% CI | a PI | IC50 | 95% CI | PI | IC50 | 95% CI | PI | |||
18 | py | 2-pic | 14.5 | 12.7–16.7 | 7.3 d | 15.5 | 11.2–21.5 | 5.3 d | ND | ND | ND |
19 | py | 3-pic | 4.0 | 3.0–5.4 | >51.5 | 3.3 | 1.9–5.9 | >71.0 | 5.5 | 3.2–9.4 | >38 |
20 | py | 4-pic | 5.4 | 4.3–6.8 | >38 | 4.6 | 3.8–5.6 | >45 | 12.3 | 7.9–19.1 | >17 |
23 | 3-pic | 3-pic | 7.2 | 6.0–8.7 | >27.8 | 10.4 | 8.7–12.2 | >19.3 | ND | ND | ND |
26 | 4-pic | 4-pic | 2.1 | 1.6–2.7 | >95 | 4.1 | 3.3–5.1 | >48.8 | 8.2 | 5.5–12.0 | >24 |
29 | Thiazole | Thiazole | 2.4 | 2.2–2.7 | 48 d | 2.9 | 1.6–5.2 | >71.0 | 7.6 | 5.4–10.7 | >27 |
32 | mim | mim | 56.3 | 40.2–78.9 | >3.7 | 164.2 | Wide | >1.3 | ND | ND | ND |
FM165 c | py | NH3 | 25.4 | 22.2–29.1 | >9.6 | b ND | ND | ND | ND | ND | ND |
3 | py | py | 6.7 | 3.6–13.7 | >45 | ND | ND | ND | 8.4 | ND | >45 |
aPI = phototoxic index (ratio of cytotoxicity following irradiation vs. in the dark). Explicit cytotoxicity values in the dark will be added to the ESI if they become available.
bND = not determined.
cFM165 = trans,trans,trans-[Pt(N3)2(OH)2(NH3)(py)].
d= cytotoxic in the absence of irradiation. mim = 1-methylimidazole.