Table 3.

In vitro antimalarial activity of prodiginines containing aryl substituents at either the 3, or the 3 and 5 positions, of the terminal pyrrole ring

Compd	R1	R2	IC50 (nM)		Cytotoxicity (nM)
			D6	Dd2
CQ	-	-	11	135	16057
39	H	C6H5CH2	83	86	< 125
40	H	4-OCH3C6H4CH2	170	156	< 125
41	H	4-ClC6H4CH2	65	81	< 125
42	H	4-BrC6H4CH2	90	108	< 125
43	H	2-NaphthylCH2	56	N.D.	N.D.
56	C2H5	4-ClC6H4CH2	6.3	6.2	< 125
57	n-C3H7	4-ClC6H4CH2	3.0	2.6	< 125
58	n-C6H13	4-ClC6H4CH2	2.0	1.8	< 125
59	n-C7H15	4-ClC6H4CH2	2.8	2.2	< 125
60	n-C8H17	4-ClC6H4CH2	16.0	12.0	1105
61	4-ClC6H4CH2		3.9	2.9	1007
62	n-C6H13	4-FC6H4CH2	0.9	0.9	1462
63	n-C8H17	4-FC6H4CH2	1.3	1.2	< 125
64	n-C6H13	4-BrC6H4CH2	2.9	2.8	< 125
65	n-C8H17	4-BrC6H4CH2	4.0	2.9	< 125
66	4-ClC6H4CH2	4-ClC6H4CH2	6.1	4.8	< 125
67	4-FC6H4CH2	4-FC6H4CH2	5.6	5.7	< 125
68	4-BrC6H4CH2	4-BrC6H4CH2	14.0	11.0	< 125
69	4-FC6H4CH2	4-ClC6H4CH2	6.1	6.1	< 125
70	4-BrC6H4CH2	4-ClC6H4CH2	8.3	7.7	< 125
71	4-BrC6H4CH2	4-FC6H4CH2	5.7	5.1	< 125
72	2,4-Cl2C6H3CH2	2,4-Cl2C6H3CH2	12.6	11.0	< 125
73	2,6-F2C6H3CH2	2,6-F2C6H3CH2	14.7	18.3	< 125
74	3-FC6H4CH2	3-FC6H4CH2	5.1	6.7	< 125
75	2-ClC6H4CH2	2-ClC6H4CH2	3.6	4.9	< 125

N.D.: not determined