| Autor: |
Kravchenko, D. V., Kuzovkova, Y. A., Kysil, V. M., Tkachenko, S. E., Maliarchouk, S., Okun, I. M., Balakin, K. V., Ivachtchenko, A. V. |
| Zdroj: |
Journal of Medicinal Chemistry; June 2005, Vol. 48 Issue: 11 p3680-3683, 4p |
| Abstrakt: |
Synthesis, biological evaluation, and SAR dependencies for a series of novel 1,3-dioxo-2,3-dihydro-1H-pyrrolo[3,4-c]quinoline inhibitors of caspase-3 are described. The inhibitory activity of the synthesized compounds is highly dependent on the nature of 4-substituents on the core scaffold. 4-Methyl- and 4-phenyl-substituted derivatives, which were the most active compounds within this series, inhibited caspase-3 with IC50 of 23 and 27 nM, respectively. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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