Table 2.
Inhibitors of FDFT1 classified by structure.
| Structure | Substances | IC50 (FDFT1 Inhibition) |
Assay | Reference |
|---|---|---|---|---|
| SUBSTRATE (FPP) ANALOGUES | Isoprenyl Phosphinylformates (1) | 8.7–197 μM | Rat liver microsomes | [240] |
| YM175 (2) | 64 nM | Rat liver microsomes | [231] | |
| ER-28488 (3) | 3.6 nM | Rat liver microsomes | [230] | |
| ER-27856 (4) (prodrug of ER-28488) |
39 μM | Rat liver microsomes | [230] | |
| BENZOXAZEPINES | TAK-475 (Lapaquistat) (5) | 78 nM | HepG2 cells | [241] |
| TRANSITION- STATE ANALOGUES | Aza analogues (6) | 3–10 μM | Yeast microsomes (In the presence of PPi) |
[242] |
| N-(arylalkyl) farnesylamine derivative (7) | 0.05 μM | Rat liver microsomes | [243] | |
| RPR 101821 (8) | 1 nM | Rat liver microsomes | [231] | |
| Aziridine diphosphate (9) | 1.2–1.9 μM | Yeast microsomes (In the presence of PPi) |
[244] | |
|
ZARAGOZIC ACIDS
(SQUALESTATINS) |
Zaragozic acid A (10) | 6 μM | HepG2 cells | [229] |
| Zaragozic acid B (11) | 0.6 μM | |||
| Zaragozic acid C (12) | 4 μM | |||
| DICARBOXYLIC ACID DERIVATIVES | Schizostatin (13) | 0.84 μM | Unknown | [233] |
| J-104,118 (14) | 0.52 nM | Hep G2 cells | [245] | |
| J-104,123 (15) | 2.5 nM | Hep G2 cells | [246] | |
| A-87049 (16) | 37 nM | Rat liver microsomes | [247] | |
| PROPYLAMINE DERIVATIVES | YM-75440 (17) | 63 nM | Hep G2 cells | [248] |
| QUINUCLIDINE DERIVATIVES | ZM-97480 (18) | 16 nM | Rat liver microsomes | [249] |
| RPR 107393 (19) | 0.6–0.9 nM | Rat liver microsomes | [231] | |
| YM-53601 (20) | 79 nM | Hep G2 cells | [190] | |
| MORPHOLINES | EP2306 (21) | 63 μM | Human liver microsomes | [250] |
| EP2302 (22) | 1 μM |