Table 2.
Inhibition of growth of MKN-45 human gastric cancer, MDA-MB-231 human breast cancer, PC-3 human prostate cancer, MIA PaCa-2 human pancreatic cancer, and H-345 human SCLC cell lines by DOX, 2-pyrrolino-DOX (AN-201), and their corresponding cytotoxic SST analogs
| Compound | IC50,* 10−10 M
|
||||
|---|---|---|---|---|---|
| MKN-45 at 100 hr | MDA-MB-231 at 120 hr | PC-3 at 120 hr | MIA PaCa-2 at 94 hr | H-345 at 96 hr | |
| DOX | 1,900 | 1,200 | 920 | 440 | 35,000 |
| Analogs with DOX | |||||
| AN-162† | 2,300 | 1,300 | 1,800 | 560 | 35,000 |
| AN-163‡ | 1,900 | 1,600 | 2,100 | 700 | 650,000 |
| AN-201 | 1.8 | 1.9 | 5 | 3.5 | 24 |
| Analogs with AN-201 | |||||
| AN-238† | 3.6 | 3.2 | 5 | 3.3 | 40 |
| AN-258‡ | 4.2 | 3.5 | 22 | 5.7 | 166 |
Cell growth inhibition data, determined at three different concentrations, were used to calculate the drug concentration that inhibited cell growth by 50% as compared to untreated control cultures. All data was derived from an average of three determinations each in eight replicates. The different cell lines were grown as described. The carrier peptides had no effect on cell proliferation in these assays at 10−6 M and lower concentrations.
Analogs with carrier RC-121.
Analogs with carrier RC-160.