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. 2013 Apr 22;208(3):489–499. doi: 10.1093/infdis/jit179

Table 3.

Structure Activity Relationships on the Ansamycin Scaffold

NSC Number Structure EC50 (nM)a
T. brucei L1210 Selectivityb
330500 Macbecin II graphic file with name jit17918.jpg 240 47 0.2c
265481 graphic file with name jit17919.jpg >80 000 >80 000 NA

Abbreviations: EC50, half maximal effective concentration; NA, not applicable; T. brucei, Trypanosoma brucei.

a Values are mean of at least 3 independent determinations. Coefficients of variation for EC50 values were all ≤35%. r2 values for dose-response curves all exceeded 0.98; within an assay, the coefficients of variation for quadruplicate determinations were ≤10% and averaged 2.6%.

b Defined as the ratio of the L1210 EC50 to the T. brucei EC50; large numbers are favorable.

c P < .05, by a 2-tailed t test.