Table 3. Exploration of fused rings as potential linker.
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Compound number | Ar | T. brucei a EC50 (nM) | CRL-8155 b CC50 (nM) | HepG2 c CC50 (nM) |
30 | 31 | >50 000 | >50 000 | |
31 | 24 ± 6 (n = 2) | 13 000 | >50 000 | |
32 | >2000 | ND d | ND | |
33 | 32 | >50 000 | >50 000 |
aControl for T brucei EC50 assay average ± SEM: pentamidine (1.8 ± 0.3 nM, n = 7).
bControl for CRL-8155 CC50 assay average ± SEM: quinacrine (4.8 ± 1.0 μM, n = 4).
cControl for HepG2 CC50 assay average ± SEM: quinacrine (10.0 ± 2.0 μM, n = 3).
dND: not determined.