Matrix metallo-proteinase (MMP-2) organoboronate inhibitors.
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.
Ali
Hijazi Abu
HA
Department of Medicinal Chemistry and Natural Products, Hebrew University in Jerusalem POB 12065, Jerusalem 91120, Israel.
Berkovitz
Ronny
R
Reich
Reuven
R
Srebnik
Morris
M
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
D001896:Boron Compounds; D061965:Matrix Metalloproteinase Inhibitors