| Autor: |
Tasdemir, D., Mallon, R., Greenstein, M., Feldberg, L. R., Kim, S. C., Collins, K., Wojciechowicz, D., Mangalindan, G. C., Concepcion, G. P., Harper, M. K., Ireland, C. M. |
| Zdroj: |
Journal of Medicinal Chemistry; January 2002, Vol. 45 Issue: 2 p529-532, 4p |
| Abstrakt: |
Raf/MEK-1/MAPK cascade inhibitor activity-directed fractionation of the sponge Stylissa massa afforded eight known alkaloids: aldisine (1), 2-bromoaldisine (2), 10Z-debromohymenialdisine (3), 10E-hymenialdisine (4), 10Z-hymenialdisine (5), hymenin (6), oroidin (7), and 4,5-dibromopyrrole-2-carbonamide (8). Both 4 and 5 showed significant enzyme inhibitory activity (IC50 3 and 6 nM, respectively). Secondary assays identified these compounds as potent MEK-1 inhibitors. Compounds 4 and 5 also inhibited the growth of human tumor LoVo cells. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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