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. 2016 Feb;23(6):520–577. doi: 10.2174/0929867323666151223095839

Table 22. Dainippon SAR for the C-3 position of N-1 2-thiazole quinolones: biochemical prokaryotic and eukaryotic IC50 values and cytotoxicity in a P388 murine cell line.

Scaffold Compound R3 Antibacterial activity
MIC (μg/ml)
Cytotoxicity
CC50 (μg/ml)a
E. coli
NIHJ JC-2
S. aureus
209 JC-1
murine P388b
130 -CO2H 0.025 0.39 0.02
169 -H 12.5 12.5 0.18
170 -CONH2 >100 >100 0.27
11 -CO2H
vosaroxin
1.56 3.13 0.01
171 -CH2OH >100 25 0.06

a Concentration that reduces cell viability by 50%; bmurine lymphocytic leukaemia cell line.