| Autor: |
Lo YH; Graduate Institute of Pharmaceutical Science, Kaohsiung Medical University, Kaohsiung, Taiwan., Lin IL, Lin CF, Hsu CC, Yang SH, Lin SR, Wu MJ |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry [Bioorg Med Chem] 2007 Jul 01; Vol. 15 (13), pp. 4528-36. Date of Electronic Publication: 2007 Apr 19. |
| DOI: |
10.1016/j.bmc.2007.04.024 |
| Abstrakt: |
A series of acyclic enediynes showing significant inhibition on the growth of tumor cancer is disclosed. To investigate the structure-activity relationship, compounds 12-33 were synthesized. Among them, compound 17 showed most potent growth inhibition activity against all tumor cell lines at low concentration, such as SR (0.4microM) and MDA-MB-435 (0.8microM), and almost completely blocked cell cycle in G2/M phase via controlling Cyclin A and Cdc25C expression. On the other hand, compound 29 showed potent induced apoptosis activity by inducing activation of caspase-3, -8, and -9. Thus, this article disclosed a new multiple-protein regulator in cell cycle regulation and induced apoptosis to achieve the goal of anticancer drug. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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