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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 4.

T. brucei and HepG2 growth inhibition data for focused analogs of 10a.

graphic file with name nihms-471692-f0041.jpg
Entry Compd position R1 Tbb EC50 (μM)a,b HepG2 IC50 (uM)
1 10a p graphic file with name nihms-471692-t0042.jpg 1.39 >15
2 10k m graphic file with name nihms-471692-t0043.jpg 0.33 > 15
3 10l p graphic file with name nihms-471692-t0044.jpg 0.32 > 15
4 10m m graphic file with name nihms-471692-t0045.jpg 0.46 >15
5 10n p graphic file with name nihms-471692-t0046.jpg 0.35 > 15
6 10o m graphic file with name nihms-471692-t0047.jpg 0.25 > 15
7 10p p graphic file with name nihms-471692-t0048.jpg 0.53 > 15
8 10q p graphic file with name nihms-471692-t0049.jpg 0.81 1.81
9 10r p graphic file with name nihms-471692-t0050.jpg 0.47 > 15
10 10s p graphic file with name nihms-471692-t0051.jpg 0.28 3.32
11 10t p CH3 0.90 > 15
12 10u m CH3 3.21 > 15
13 10v o N(CH3)2 1.04 > 15
14 10w o NHC(CH3)3 4.66 ndc
a

All EC50 values are ± 7%.

b

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

c

Not determined.