title: Matrix metallo-proteinase (MMP-2) organoboronate inhibitors.
abstract: Novel organoboronate derivatives consisting of BB, BC(R(1)R(2))B, BCCB, CBC, Department of Medicinal RBC=CBB, and RBC=CBP structures were synthesized and have been investigated in vitro as MMP-2 inhibitors. We discovered that most of the boronate derivatives (those not containing phosphorus) showed significant activity against MMP-2. The trisboronate 14 proved to be a potent MMP-2 inhibitor at 5 and 10 microM. Structure activity relationships (SARs) data for the compounds were investigated and are discussed.
authors.affiliation: Department of Medicinal Chemistry and Natural Products, Hebrew University in Jerusalem POB 12065, Jerusalem 91120, Israel.
authors.forename: Hijazi Abu
authors.initials: HA
authors.lastname: Ali
authors.forename: Ronny
authors.initials: R
authors.lastname: Berkovitz
authors.forename: Reuven
authors.initials: R
authors.lastname: Reich
authors.forename: Morris
authors.initials: M
authors.lastname: Srebnik
mesh_terms: D001485:Basement Membrane / Q000187:drug effects; D001896:Boron Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D061965:Matrix Metalloproteinase Inhibitors; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D001896:Boron Compounds; D061965:Matrix Metalloproteinase Inhibitors