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. 2010 Jan;169(1):12–19. doi: 10.1016/j.molbiopara.2009.09.002

Table 3.

Potency of representative compounds against trypanothione reductase from T. b. brucei and T. cruzi and growth inhibition of T. b. brucei cells. All IC50 values against TbTryR and TcTryR were determined in the 412 nm assay on three separate occasions. IC50 values were determined with T(S)2 at S = Km (2.35 μM for TbTryR and 10.4 μM for TcTryR). For structures see Fig. 4. Linear regression analysis of IC50 for TbTryR versus EC50 for T. brucei yielded a regression coefficient of r2 = 0.49.

Compound IC50 (μM)
 Ratio EC50 (μM)
TbTryR TcTryR Tc/Tb T. b. brucei
Ebselen 0.18 ± 0.01 0.60 ± 0.01 3.3 2.97a
DM8a 3.17 ± 0.17 7.99 ± 0.51 2.5 1.00 ± 0.21b
DM6a 3.20 ± 0.16 3.80 ± 0.20 1.2 0.68 ± 0.10b
DM5a 6.80 ± 0.42 16.9 ± 1.08 2.5 0.55 ± 0.04b
Thioridazine 9.58 ± 0.38 10.0 ± 0.31 1.0 1.39 ± 0.03
Clomipramine 11.1 ± 0.42 3.41 ± 0.06 0.3 5.04a
DM7a 19.2 ± 1.75 27.8 ± 2.08 1.4 3.01 ± 0.3b
Quinacrine 22.1 ± 2.05 37.8 ± 1.91 1.7 n.d.
Trifluoperazine 40.5 ± 1.50 20.9 ± 0.90 0.5 2.11 ± 0.50
Citalopram 82.3 ± 6.35 154 ± 5.42 1.9 6.59 ± 0.54
a

Data from Richardson et al. [33].

b

Data from Martyn et al. [19].