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Synthesis of arylidene-substituted gelastatin analogues and their screening for MMP-2 inhibitory activity
1Department of Chemistry and Division of Molecular Life Sciences, Ewha Womans University, Seoul 120-750, Korea.
Bioorganic & Medicinal Chemistry
|May 25, 2005
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.