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. 2010 Nov 25;6(2):302–308. doi: 10.1002/cmdc.201000450

Table 2.

Activity of R3-substituted compounds against TbPTR1, TbDHFR and human DHFR, and T. brucei and MRC5 cells. R1 in all compounds is 3,4-dichlorobenzyl

Compd R3 TbPTR1 Inline graphic [μm] HsDHFR IC50 [μm] TbDHFR IC50 [μm] T. brucei[a] EC50 [μm] MRC5 EC50 [μm]
11[b] H 0.8 >50 >50 11 27
24 4-Cl 2.3 >50 >30 ND[d] ND
25 4-O(CH2)2CH3 0.31 >50 >30 ND ND
26 4-OBn 16 >50 >50 >30 >30
27 4-Ph >60 >30 >30 ND ND
28[c] 4-OMe 0.46 >50 >30 ND ND
29[b] 7-Cl 0.51 >50 >30 ND ND
30[b] 7-O(CH2)2CH3 0.047 >50 >30 9.6 21
31 7-OBn 0.098 >50 >50 6.7 17
32[b] 7-Ph 0.007 >50 >50 9.9 >30
33 7-OMe 0.65 >50 >30 ND ND
34 5,6-dimethyl 3.9 >30 >30 ND ND
[a]

In vitro cell assay conditions used were as reported previously.21

[b]

Some data for these compounds have been reported previously.13

[c]

Contaminated with ∼25 % of compound 33.

[d]

ND=Not determined.