Abstract
A series of arylidene-substituted gelastatin analogues were synthesized in a divergent manner. Each analogue was obtained as a mixture of isomers. Calculation methods were devised to deduce the MMP-2 inhibitory activity of each isomer from the activity of an isomeric mixture and its composition. This protocol is suitable for rapidly generating a variety of arylidene-substituted gelastatin analogues and screening them for highly active inhibitors.
| Original language | English |
|---|---|
| Pages (from-to) | 4103-4112 |
| Number of pages | 10 |
| Journal | Bioorganic and Medicinal Chemistry |
| Volume | 13 |
| Issue number | 12 |
| DOIs | |
| State | Published - 2 Jun 2005 |
Keywords
- Gelastatin analogues
- MMP-2 inhibitor
- Screening