Table 1.

Antileishmanial activities of aphidicolin and derivatives

CompoundaEC50 (μg/ml) against parasite:EC50 (μg/ml) for cytotoxicity to cells:SIb
L. major (extracellular)L. donovani (extracellular)L. infantum (extracellular)L. enriettii (extracellular)L. donovani (intracellular)BMMφKBSK-Mel
10.190.540.140.310.12>25.0>25.0>25.0208
21.772.501.701.880.95>25.0>25.0>25.026
31.830.620.991.320.1124.9>25.0>25.0226
40.400.600.420.420.21>22.4>25.0>25.0106
50.090.080.100.100.0518.2>25.0>25.0364
60.050.040.060.040.20>25.0>25.0>25.0125
70.510.310.500.510.36>25.0>25.0>25.069
81.090.631.701.141.11>25.0>25.0>25.023
90.380.310.950.330.20>25.0>25.0>25.0125
100.410.320.950.650.25>25.0>25.0>25.0100
110.370.270.890.610.24>25.0>25.0>25.0104
120.541.250.673.300.56>25.0>25.0>25.044
13>5.0>5.0>5.0>5.0>5.0>25.0>25.0>25.05
140.120.080.120.120.09>25.0>25.0>25.0277
150.450.660.440.570.20>25.0>25.0>25.016
161.25>5.0>5.03.30>5.0>25.0>25.0>25.05
171.251.841.880.851.51>25.0>25.0>25.016
180.120.200.210.110.0211.3>25.0>25.0565
AMB0.030.030.040.020.025>25.0>25.0>25.01,000
MF0.020.050.060.020.002>25.0>25.0>25.0<12,500
  • a AMB, amphotericin B; MF, miltefosin.

  • b SI, ratio of EC50 for cytotoxicity to BMMφ to EC50 for intracellular L. donovani.