Table 4.
Biological examination of pactamycin and synthetic analogsa
| Entry | Structure | Code number | A549 EC50 (lung cancer) |
MDA-MB-231 EC50 (breast cancer) |
SK-OV-3 EC50 (ovarian cancer) |
MRC-5 EC50 (human lung fibroblast) |
|---|---|---|---|---|---|---|
| 1 |
|
1 | 160 nM | 124 nM | 129 nM | 53 nM |
| 2 |
|
28 | 11.8 μM | 10.4 μM | 12 μM | n.t.b |
| 3 |
|
ent-(1) | 2.1 μM | 1.2 μM | 1.6 μM | 933 nM |
| 4 |
|
15a | 800 nM | 659 nM | 1.4 μM | 380 nM |
| 5 |
|
15b | 141 nM | 556 nM | 434 nM | 314nM |
| 6 |
|
15c | 1μM | n.t.b | 600 nM | 582 nM |
| 7 |
|
15d | 777 nM | 4μM | 4 μM | 682 nM |
| 8 |
|
15e | 884 nM | 3.3 μM | 1.6 μM | 2326 nM |
| 9 |
|
15f | 324 nM | 376 nM | 145 nM | 431 nM |
| 10 |
|
15g | 2.21 μM | 1.84 μM | 2.44 μM | 860 nM |
| 11 |
|
15h | 760 nM | 800 nM | 436 nM | 366 nM |
| 12 |
|
21 | 6μM | n.t.b | 3.8 μM | 2933 nM |
| 13 |
|
22a | n.t.b | n.t.b | n.t.b | n.t.b |
| 14 |
|
22b | n.t.b | n.t.b | n.t.b | n.t.b |
| 15 |
|
22c | n.t.b | n.t.b | n.t.b | n.t.b |
|
||||||
| 16 |
|
26a | n.t.b | n.t.b | n.t.b | 2063 nM |
| 17 |
|
26b | n.t.b | n.t.b | n.t. b | 10.9 μM |
| 18 |
|
26c | 32 nM | 50 nM | 7 nM | 6.5 nM |
| 19 |
|
29 | 83 nM | 356 nM | 91 nM | 49 nM |
| 20 |
|
27b | 88 nM | 203 nM | 103 nM | 129 nM |
| 21 |
|
27c | 114 nM | 79 nM | 80 nM | 105 nM |
| 22 |
|
27d | 118 nM | 300 nM | 75 nM | 100 nM |
| 23 |
|
27e | 194 nM | 352 nM | 436 nM | 366 nM |
| 24 | R = Ac | 27f | 137 nM | 458 nM | 123 nM | 132 nM |
| 25 |
|
27h | 175 nM | 1.93 μM | 86 nM | 396 nM |
| 26 |
|
27g | 588 nM | 2.44 μM | 593 nM | 778 nM |
Assays were carried out as triplicates.
Not toxic.