. 2012 Mar 13;52:82–97. doi: 10.1016/j.ejmech.2012.03.007

Table 2.

In vitro anti-plasmodial activity, cytotoxicity, resistance factor and selectivity index of compounds 10a-s.

Compound	IC₅₀ (nM)		Resistance factor^e	ClogP^f	Cytotoxicity (μM)^g		Selectivity index^j
Compound	CQ^S (3D7)^a^,^b	CQ^R (K1)^c^,^d	Resistance factor^e	ClogP^f	CC₅₀^h	MICⁱ	Selectivity index^j
10a	21.7	139.3	6.43	6.83	1.4	0.8	10.04
10b	247.5	52.2	0.210	6.82	0.8	0.8	15.33
10c	202.3	26.1	0.129	7.35	0.9	0.8	34.41
10d	1134.9	617.7^b	0.544	8.94	–	–	–
10e	252.2	516.4	2.047	9.47	–	–	–
10f	1776.8	487.7	0.2744	10.53	–	–	–
10g	264.8	853.7	3.22	11.58	–	–	–
10h	14828.3	27320.9	1.842	8.81	–	–	–
10i	644.4	6186.4^b	9.600	8.80	–	–	–
10j	15888.5	28096.7	1.7683	5.31	–	–	–
10k	286.7	860.4^b	3.00	8.28	–	–	–
10l	63.1	160.8	2.5480	5.64	58.2	20	361.89
10m	42.1	1659.8^b	39.422	5.75	0.8	4	0.48
10n	598.7	230.5^b	0.385	7.30	0.5	0.8	2.1
10o	697.2	192.1	0.2756	7.30	–	–	–
10p	172.9	96.0	0.5555	6.89	2.2	≥0.8	22.90
10q	1955.1	229.3	0.1173	7.30	–	–	–
10r	18.2	3.6	0.2	7.30	2.3	4.0	638
10s	499.9	175.8	0.3518	7.30	–	–	–
2	1.4	201.8	140.39	5.1	–	–	–
Artesunate	5.3	2.8	0.5418	1.06	–	–	–

CQ sensitive strain.

primary screening.

CQ resistant strain.

secondary screening.

calculated by dividing IC₅₀ values of PFK1 by PF3D7.

calculated from Chem draw Ultra 11.0.

determined on Madin Darby canine kidney (MDCK)cells.

50% cytotoxic concentration, as determined by measuring the cell viability with the colorimetric formazan- based MTS assay (reference drugs used: Oseltamivir carboxylate CC₅₀/MIC >100, Ribavirin CC₅₀/MIC >100, Amantadine CC₅₀/MIC >200 and Rimantadine CC₅₀/MIC >200).

ⁱ

minimum compound concentration that causes a microscopically detectable alteration of normal cell morphology.

Selectivity Index (S.I.) is calculated as CC₅₀/IC₅₀ (K1 Strain) ratio.