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.

Organo-boron compoundsOrgano-boron compounds S 0040 Matrix Metallo-Proteinase (MMP-2) Organoboronate Inhibitors. -A variety of novel organoboronate derivatives are synthesized and evaluated for their MMP-2 inhibition. The trisboronate (Ic) proves to be a potent MMP-2 inhibitor. Structure-activity relationship data for the compounds are investigated and discussed. -(ALI, H. A.; BERKOVITZ, R.; REICH, R.; SREBNIK*, M.; Arch.