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. Author manuscript; available in PMC: 2019 Jul 5.
Published in final edited form as: J Med Chem. 2018 Feb 9;61(4):1450–1473. doi: 10.1021/acs.jmedchem.7b00738

Table 4.

4(1H)-Quinolones Substituted in 6-Position with the Piperazine Moiety

graphic file with name nihms-1033695-t0036.jpg
compd R EC50 W2
(nM)a 		EC50 TM90-
C2B (nM)		 RIb EC50 Pb
(nM)		 EC50
J774
(μM)
8af −H 150 >2000 >13  91 >20
 8ag −OCH3 160 >2000 >12 >100 >20
 8ah −F 110 >2000 >18 c >20
8ai −CF3   45 >2000 >44  85 >20
a

Chloroquine (CQ), atovaquone (ATO), and dihydroartemisinin (DHA) are internal controls for each in vitro assay: CQ, 0.42 μM W2, 0.23 μM TM90-C2B, and 47.2 μM J774; ATO, 1.4 nM W2, 18 μM TM90-C2B, and 28 μM J774; DHA, 5.5 nM W2, 5.9 nM TM90-C2B, and 1.5 μM J774.

b

RI = TM90-C2B/W2.

c

Not determined.