Table 1. Structures and associated in vitro testing results for N-ethyl substituted analogs of compound 1.
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Compound number | Ar | T. brucei a EC50 (nM) | CRL-8155 b CC50 (nM) | HepG2 c CC50 (nM) |
2 | 40 | >50 000 | >50 000 | |
3 | >2000 | >50 000 | >50 000 | |
4 | 31 ± 4 (n = 2) | 45 000 | >50 000 | |
5 | 26 ± 3 (n = 4) | 41 000 | 40 600 | |
6 | 210 | >50 000 | >50 000 | |
7 | 69 | 27 100 | 45 300 | |
8 | 1600 | 38 200 | 43 700 | |
9 | 660 | 31 600 | 31 300 | |
10 | 220 | 20 900 | 29 800 | |
11 | 110 | >50 000 | >50 000 | |
12 | >2000 | >50 000 | >50 000 | |
13 | 17 ± 3 (n = 2) | >50 000 | >50 000 | |
14 | 390 | >50 000 | >50 000 | |
15 | 1.6 ± 0.2 (n = 5) | >50 000 | >50 000 | |
16 | 3.4 ± 0.1 (n = 3) | >50 000 | >50 000 |
aControl for T brucei EC50 assay average ± SEM: pentamidine (1.7 ± 0.2 nM; n = 14). Compounds with initial EC50 < 30 nM were tested more than once and their EC50s are shown as average ± SEM (number of tests).
bControl for CRL-8155 CC50 assay average ± SEM: quinacrine (7.0 ± 3.7 μM; n = 3).
cControl for HepG2 CC50 assay average ± SEM: quinacrine (7.6 ± 0.9 μM; n = 5).