Table 2.

Potency and Selectivity of VS Inhibitors Designed Based on Substrate Screening Data^a,b

No.	Cap	R3	R2	R1	72 h EC50 (μM)			1 h EC50 (μM)
					Pf	HFF	SI	Pf	HFF	SI
11					0.359 ± 0.042	78.41 ± 18.01	218	nd	nd	nd
12					0.021 ±0.005	13.96 ±3.58	652	1.013 ±0.169	>250
13					0.018 ±0.005	8.54 ±2.00	482	0.33 ± 0.047	>250
14					0.008 ± 0.002	9.80 ±2.96	1240	0.137 ± 0.095	>250
15					0.035 ±0.009	15.77 ±3.51	445	8.03 ±1.33	>250
16					0.007 ±0.002	7.4 ±1.50	1138	0.051 ± 0.006	207 ±23.2	4043
17					0.369 ±0.125	246 ±49.63	667	>2.5	>250

^aEC₅₀ values for inhibitors 11–17 in 72 and 1 h treatment of P. falciparum W2 at ring stage parasites and non-confluent HFFs.

^bSI, selectivity index; nd, not determined.