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Table 1 Effects of chalcones on cultured T. b. brucei , purified trypanopain-Tb, and sheep cathepsin L

From: Chalcone, Acyl Hydrazide, and Related Amides Kill Cultured Trypanosoma brucei brucei

Compound

A

B

CLogP

T. b. brucei IC50 (µM)

Trypanopain Ki (µM)a

Cathepsin L Ki (µM)a

MC153

3.295

4.79

NIb

12.11 ± 1.41

MC135

4.245

5.49

NI

9.55 ± 1.42

MC131b

5.252

13.80

0.37 ± 0.06

7.16 ± 0.62

MC151

4.302

9.07

9.65 ± 0.91

9.48 ± 1.59

MC159

4.455

3.52

NI

4.57 ± 0.55

JD159

4.115

1.88

17.14 ± 1.76

6.95 ± 0.80

MC161

3.505

0.24

NI

40.72 ± 4.81

MC143

5.937

3.50

2.25 ± 0.29

2.66 ± 0.62

  1. a Data reflect the mean Ki ± SD (n = 3).
  2. b No inhibition.