Table 1. Summary of the biological effects of selected compounds.
| Apoptosis supported by
|
|||||||||
|---|---|---|---|---|---|---|---|---|---|
| No. | Compound NSC no. | Compound name | p53* | BAX† | Induction of p53 | DNA damage | Cytoplasmic target | LMP‡ | ER stress§ |
| 1 | 69187 | 9-methoxy-ellipticine | + | + | ++ | – | – | – | – |
| 2 | 622627 | + | + | + | + | + | – | – | |
| 3 | 102811 | Formycin A | + | + | + | + | – | – | – |
| 4 | 72961 | 8-azaadenosine | + | + | + | + | – | – | – |
| 5 | 93419 | Steffimycin | + | + | ++ | + | – | – | – |
| 6 | 651079 | – | + | ++ | + | + | + | – | |
| 7 | 687852 | – | + | + | + | + | + | – | |
| 8 | 106408 | Anthramycin meth.-ether | – | + | + | + | – | – | – |
| 9 | 267461 | Nanaomycin | – | + | + | – | + | + | – |
| 10 | 13973 | Acridine yellow | – | + | ++ | – | + | – | – |
| 11 | 166381 | – | + | – | – | – | – | – | |
| 12 | 24819 | β-Peltatin A | – | + | ++ | – | – | – | – |
| 13 | 10010 | – | + | + | – | + | – | – | |
| 14 | 647889 | – | + | + | – | + | + | – | |
| 15 | 285116 | Siomycin A | – | + | + | – | + | + | + |
| 16 | 313981 | Gold Cl-3-ethylphosphine | – | + | + | + | + | + | – |
| 17 | 140377 | Arnebin | – | + | + | – | + | – | – |
| 18 | 157389 | – | + | – | – | + | – | – | |
| 19 | 85236 | Helenalin | – | + | – | – | + | + | – |
| 20 | 24818 | Podophyllotoxin | – | + | + | – | – | – | – |
*
p53-supported apoptosis was defined as 2-fold higher CK18 cleavage in HCT116 WT cells (area under curve in Fig. 2)
†
Drugs that showed Bax-supported apoptosis induced <10% caspase activation in HT116 Bax (null) cells compared with HCT116 control cells
‡
See Fig. 5 for details
§
ER, endoplasmic reticulum. Induction of GRP78 in HCT116 p53 WT cells; cleavage of caspase-12 in mouse CT51 cells