acetyl-aspartyl-glutamyl-valyl-aspartal has been researched along with 1-2-benzisothiazoline-3-one* in 1 studies
1 other study(ies) available for acetyl-aspartyl-glutamyl-valyl-aspartal and 1-2-benzisothiazoline-3-one
| Article | Year |
|---|---|
Design, synthesis and evaluation of 1,2-benzisothiazol-3-one derivatives as potent caspase-3 inhibitors.
A number of 1,2-benzisothiazol-3-one derivatives were prepared through structural modification of the original compound from high-throughput screening. Some analogues (e.g., 6b, 6r, 6s and 6w) were identified as novel and potent caspase inhibitors with IC50 of nanomolar. Structure-activity relationship (SAR) studies for caspase-3 inhibition were evaluated in vitro. Molecular modeling studies provided further insight into the interaction of this class of compounds with activated caspase-3. The present small molecule caspase-3 inhibitor with novel structures different from structures of known caspase inhibitors revealed a new direction for therapeutic strategies directed against diseases involving abnormally up-regulated apoptosis. Topics: Caspase 3; Caspase Inhibitors; Drug Design; Enzyme Assays; High-Throughput Screening Assays; Humans; Molecular Docking Simulation; Recombinant Proteins; Structure-Activity Relationship; Thiazoles | 2013 |