Table 4. Additional inhibitors with 2,5-substituted imidazo[1,2-a]pyridine linker.
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Compound number | Ar | R | T. brucei a EC50 (nM) | CRL-8155 b CC50 (nM) | HepG2 c CC50 (nM) |
34 | Cl | 1900 | ND d | ND | |
35 | Cl | 64 | 16 100 | 43 200 | |
36 | Cl | 196 | ND | ND | |
37 | Cl | 1780 | ND | ND | |
38 | Cl | >2000 | ND | ND | |
39 | Cl | 3.5 ± 0.1 (n = 2) | 9500 | >50 000 | |
40 | Cl | 3.1 ± 0.5 (n = 6) | 19 000 | 28 200 | |
41 | F | 59 | 15 700 | >50 000 | |
42 | F | 8.4 ± 3.1 (n = 2) | 10 400 | >50 000 | |
43 | F | 7.2 ± 1.7 (n = 4) | >25 000 | >25 000 |
aControl for T brucei EC50 assay average ± SEM: pentamidine (2.4 ± 0.3 nM; n = 10).
bControl for CRL-8155 EC50 assay average ± SEM: quinacrine (6.1 ± 0.6 μM; n = 5).
cControl for HepG2 EC50 assay average ± SEM: quinacrine (10.9 ± 1.1 μM; n = 4).
dND: not determined.