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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 5.

Growth inhibitory potency of regiochemical and linker analogs of 10.

graphic file with name nihms-471692-f0052.jpg
Entry Compd R Regio X Tbb EC50 (μM)a,b HepG2 IC50 (μM)
1 23a graphic file with name nihms-471692-t0053.jpg m -- 0.042 >20
2 23b p -- 1.91 9.6
3 23c m CH2 0.36 ndc
4 23d p CH2 0.99 12.9
5 23e m C=O 0.55 nd
6 23f p C=O 1.21 nd
7 10k m SO2 0.33 >20
8 10a p SO2 1.39 >20
9 23g graphic file with name nihms-471692-t0054.jpg m -- 0.76 >15
10 23h p -- 0.38 nd
11 23i m CH2 0.65 nd
12 23j p CH2 1.5 nd
13 23k m C=O 0.14 >6
14 23l p C=O 0.94 nd
15 10m m SO2 0.46 >20
16 10l p SO2 0.32 >20
a

All EC50 values are ± 7%.

b

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

c

Not determined.