Table 1. Inhibition of the NorA-Mediated Efflux of EtBr in SA-1199B Cells and of the Pgp-Mediated Cell Efflux of R123 in Mouse T Lymphoma L5178 MDR1 Cells.
Cpd IDa | common name | % inhibition of EtBr efflux | % inhibition of R123 efflux |
---|---|---|---|
1b | reserpine | 84.8c | N.A. |
2 | amlodipine | 60.6 | 52.8d |
3 | astemizole | 80.6 | 12.8d |
4 | dipyridamole | 42.3 | 4.7e |
5 | loperamide | 77.7 | 4.5d |
6 | quinidine | 31.5 | 21.1e |
7 | aripiprazole | 92.3 | 99e,f |
8 | ebastine | 88.3 | 99e,f |
9 | sertindole | 81.8 | 74e,f |
10 | ziprasidone | 86.6 | 19e,f |
11 | aprindine | 51.6 | 16e,f |
12 | repaglinide | 14.0 | 35e,f |
13g | cyclosporine A | N.A. | 92e,f |
14h | alprenolol | N.A. | 5.0e,f |
15 | 22.8i | 44.1e | |
16 | 23.6i | 64.7e | |
17 | 33.9j | 1.9e | |
18 | 1.7j | 2.6d | |
19 | 4.4j | 3.2e | |
20 | 91.2k | 40.6e | |
21 | 19.7f | 16.8e | |
22 | 88.2c | 4.3e | |
23 | 88.4c | 1.6e | |
24 | 0c | 2.3e | |
25 | 30.6c | 21.7e | |
26 | 86.6c | 7.8d | |
27 | 0c | 2.2e | |
28 | 2.8c | 2.1e | |
29 | 71.7c | 0.6d | |
30 | 41.8c | 2.6e | |
31 | 41.3c | 20.4e | |
32 | 81.0c | 0.7d | |
33 | 15.5c | 2.6e | |
34 | 74.7c | 1.7d | |
35 | 0c | 11.3e |
Structures for compounds 1–35, IUPAC names for compounds 15–35, and SMILES are given as Supporting Information.
Reserpine was used as a positive control for EtBr efflux inhibition.
From ref (16).
Tested at 10–5 M concentration.
Tested at 10–4 M concentration.
From ref (18).
Cyclosporine A was used as a positive control for R123 efflux inhibition.
Alprenolol was used as a negative control for R123 efflux inhibition.
From ref (21).
From ref (22).
From ref (17).