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. Author manuscript; available in PMC: 2016 Dec 11.
Published in final edited form as: ACS Infect Dis. 2015 Aug 2;1(12):604–614. doi: 10.1021/acsinfecdis.5b00063

Table 2.

In Vitro Characterization of Representative Compounds

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
a

Nuclear morphology/membrane permeability/mitochondrial potential.

b

Data from Nixon et al.15

c

nd, not determined.