Table 1.

Potency and Selectivity of P1 and P3 Bulky Aromatic VS Inhibitors^a,b

No.	Cap	R3	R2	R1	72 h EC50 (μM)			1 h EC50 (μM)
					Pf	HFF	SI	Pf	HFF	SI
WLL -vs					0.015 ± 0.005	1.52 ±0.41	101	0.147 ± 0.009	65.50 ± 15.2	446
1					0.010 ± 0.002	1.80 ±0.39	178	0.061 ±0.011	nd	nd
2					0.090 ±0.016	1.67 ±0.26	19	0.495 ± 0.058	nd	nd
3					0.003 ± 0.0006	1.88 ±0.46	570	0.048 ± 0.006	75.65 ± 12.68	1576
4					0.191 ± 0.036	1.67 ±0.32	9	6.27 ±2.64	135 ±42.2	21.5
5					0.062 ±0.013	1.01 ±0.16	16	2.03 ±0.34	nd	nd
6					1.207 ± 0.093	> 100		nd	nd	nd
7					0.022 ± 0.005	13.38 ±4.41	600	0.32 ± 0.035	>250
8					0.015 ± 0.002	2.08 ±0.46	138	0.091 ± 0.028	nd	nd
9					0.002 ± 0.0002	0.31 ± 0.098	172	0.008 ± 0.002	11.4 ±2.2	1443
10					0.009 ± 0.002	4.36 ± 1.04	464	0.081 ±0.013	124 ±42.3	1536
					0.030 ± 0.008	2.75 ±0.50	92	0.342 ± 0.074	>50

^aEC₅₀ values for each of the inhibitors 1–10 and the Carmaphycin B analog in 72 and 1 h treatment of P. falciparum W2 at ring stage parasites and non-confluent HFFs.

^bSI, selectivity index; nd, not determined.