Skip to main content
. 2020 May 18;11(8):885–895. doi: 10.1039/d0md00057d

Table 1. Structures and associated in vitro testing results for N-ethyl substituted analogs of compound 1.

Inline graphic
Compound number Ar T. brucei a EC50 (nM) CRL-8155 b CC50 (nM) HepG2 c CC50 (nM)
2 graphic file with name d0md00057d-u2.jpg 40 >50 000 >50 000
3 graphic file with name d0md00057d-u3.jpg >2000 >50 000 >50 000
4 graphic file with name d0md00057d-u4.jpg 31 ± 4 (n = 2) 45 000 >50 000
5 graphic file with name d0md00057d-u5.jpg 26 ± 3 (n = 4) 41 000 40 600
6 graphic file with name d0md00057d-u6.jpg 210 >50 000 >50 000
7 graphic file with name d0md00057d-u7.jpg 69 27 100 45 300
8 graphic file with name d0md00057d-u8.jpg 1600 38 200 43 700
9 graphic file with name d0md00057d-u9.jpg 660 31 600 31 300
10 graphic file with name d0md00057d-u10.jpg 220 20 900 29 800
11 graphic file with name d0md00057d-u11.jpg 110 >50 000 >50 000
12 graphic file with name d0md00057d-u12.jpg >2000 >50 000 >50 000
13 graphic file with name d0md00057d-u13.jpg 17 ± 3 (n = 2) >50 000 >50 000
14 graphic file with name d0md00057d-u14.jpg 390 >50 000 >50 000
15 graphic file with name d0md00057d-u15.jpg 1.6 ± 0.2 (n = 5) >50 000 >50 000
16 graphic file with name d0md00057d-u16.jpg 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).