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. Author manuscript; available in PMC: 2017 Feb 1.
Published in final edited form as: Bioorg Med Chem Lett. 2015 Dec 22;26(3):854–857. doi: 10.1016/j.bmcl.2015.12.080

Table 2.

Comparison of selectivity indexes of compounds 1–6 with CQ and RMP

Compound IC50 Vero cell µM SIa SIb SIc
1 99.74 32174 83117 10.2
2 >100 >9 >8 >1.0
3 and 4d 78.14 545 253 2.9
5 48.55 7356 19420 12.4
6 95.22 639 505 45.3
CQ 234.47e 4518 21511 –
RMP >100 – – >1100
a

Selectivity index (SI) defined by the ratio: IC50 (in mammalian Vero cell lines)/IC50 of antiparasitic activity against Dd2 (CQ-resistant strain) cell line.

b

Selectivity index (SI) defined by the ratio: IC50 (in mammalian Vero cell lines)/IC50 of antiparasitic activity against 3D7 (CQ-sensitive strain) cell line.

c

Selectivity index (SI) defined by the ratio: IC50 (in mammalian Vero cell lines)/MIC of antimycobacterial activity against M. tuberculosis H37Rv cell line.

d

Tested as a 2:3 mixture of regioisomers.

e

Value obtained from Ref. 24.

CQ = chloroquine and RMP = rifampicin (+Ctrls).