title: Synthesis of arylidene-substituted gelastatin analogues and their screening for MMP-2 inhibitory activity.
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.
authors.affiliation: Department of Chemistry and Division of Molecular Life Sciences, Ewha Womans University, Seoul 120-750, Korea.
authors.forename: Eun Jin
authors.initials: EJ
authors.lastname: Kim
authors.forename: Soo Y
authors.initials: SY
authors.lastname: Ko
mesh_terms: 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
chemical_list: D061965:Matrix Metalloproteinase Inhibitors; D011422:Propionates; D011753:Pyrones; C106757:gelastatin A; C106758:gelastatin B; D018093:Gelatinases