Synthesis of arylidene-substituted gelastatin analogues and their screening for MMP-2 inhibitory activity.
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.
Kim
Eun Jin
EJ
Department of Chemistry and Division of Molecular Life Sciences, Ewha Womans University, Seoul 120-750, Korea.
Ko
Soo Y
SY
D045744:Cell Line, Tumor; D018093:Gelatinases / Q000037:antagonists & inhibitors; D006801:Humans; D007536:Isomerism; D061965:Matrix Metalloproteinase Inhibitors; D011422:Propionates / Q000138:chemical synthesis*; D011753:Pyrones / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
D061965:Matrix Metalloproteinase Inhibitors; D011422:Propionates; D011753:Pyrones; C106757:gelastatin A; C106758:gelastatin B; D018093:Gelatinases