Table 2.
Compd | NCI-H460[c] | NCI-H520[d] | NCI-H522[d] | NCI-H1435[d] | A549[c] | pKa |
---|---|---|---|---|---|---|
P1–A1 | 0.0052±0.0001 (520)[e] | 0.043±0.004 (100) | 0.010±0.001 | 0.84±0.07 | 0.0065±0.0002 | 9.4±0.2 |
P1–B1 | 0.24±0.01 (3.8) | 0.52±0.01 (3.5) | 0.12±0.02 | 1.48±0.01 | 0.32±0.06 | 7.6±0.3 |
P1–B2 | 2.4±0.5 (0.9) | 2.2±0.1 (1.5) | 3.62±0.08 | 11.0±0.2 | 12.4±0.9 | 4.9±0.6 |
Concentrations of compound that reduce cell viability by 50%, extracted from dose-response curves for 72 h drug incubations using a colorimetric (MTS) cell proliferation assay. Values are means of two individual experiments performed in triplicate ±standard deviations.
Determined from Henderson-Hasselbalch plots of UV-visible absorbance data (averages for three titrations ±standard deviations; see the Supporting Information).
Wild-type p53.
Mutated p53.
Values in parentheses are enhancement factors relative to Pt-free ligands A1, B1, and B2 (see Supporting Information).