Table 2.
compound | enzyme IC50 (nM) |
MIC90 (µM) |
Tox50 (µM) |
selectivity index (Tox50/MIC90) | intracell MIC90 (µM) | cell healtha (µM) | ||
---|---|---|---|---|---|---|---|---|
Mtb | human | wt | DHFR-oe | HepG2 | ||||
WR99210 | 14a | 9.0 | 1–2 | 15–30 | 40 | 20 | 9.7 | 10/19/25 |
PDP-1 | 8.2 | 6.7 | 1.25 | 30 | 40 | 32 | 1.2 | ndc |
PQD-1 | 7.1 | 6.8 | 0.50 | >2 | 10 | 20 | 0.7 | nd |
DPt-1 | 49.1 | 382.1 | 2–8 | 250 | >50 | >17 | 28 | 200/200/200 |
DQn-1 | 6.2 | 7.6 | 0.03 | 1.0 | >50 | >1000 | 0.05 | 200/200/200 |
trimetrexateb | 17 | nd | 6.25 | >100 | nd | nd | nd | nd |
Nuclear morphology/membrane permeability/mitochondrial potential.
Data from Nixon et al.15
nd, not determined.