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. Author manuscript; available in PMC: 2014 May 23.
Published in final edited form as: J Med Chem. 2013 May 3;56(10):3820–3832. doi: 10.1021/jm400349k

Table 3.

T. brucei growth inhibition data for headgroup variations of 10a.

graphic file with name nihms-471692-f0028.jpg
Compd R1 R2 Tbb EC50 (μM)a,b HepG2 IC50 (uM)
10a graphic file with name nihms-471692-t0029.jpg Cl 1.39 >15
20a H H 1.44 > 3
20b CH3 H 1.15 > 15
20c OH Cl 1.06 > 15
20d OCH3 Cl 0.82 > 15
20e graphic file with name nihms-471692-t0030.jpg Cl 1.35 > 15
20f graphic file with name nihms-471692-t0031.jpg Cl 0.68 > 15
20g graphic file with name nihms-471692-t0032.jpg Cl 0.66 > 15
20h graphic file with name nihms-471692-t0033.jpg Cl 0.82 >15
20i graphic file with name nihms-471692-t0034.jpg Cl 1.65 > 15
20j graphic file with name nihms-471692-t0035.jpg Cl 1.34 > 15
20k graphic file with name nihms-471692-t0036.jpg Cl 1.43 > 15
20l graphic file with name nihms-471692-t0037.jpg Cl 0.54 > 15
20m graphic file with name nihms-471692-t0038.jpg Cl 1.12 > 3
20n graphic file with name nihms-471692-t0039.jpg H 0.65 > 15
20o graphic file with name nihms-471692-t0040.jpg OCH3 1.88 > 15
a

All EC50 values are ± 7%.

b

Concentration giving 50% inhibition of growth of T brucei brucei Lister 427 cells