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 |
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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