TY - JOUR
T1 - Matrix metallo-proteinase (MMP-2) organoboronate inhibitors
AU - Ali, Hijazi Abu
AU - Berkovitz, Ronny
AU - Reich, Reuven
AU - Srebnik, Morris
PY - 2004/4
Y1 - 2004/4
N2 - Novel organoboronate derivatives consisting of BB, BC(R1R 2)B, BCCB, CBC, 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 μMU. Structure-activity relationships (SARs) data for the compounds were investigated and are discussed.
AB - Novel organoboronate derivatives consisting of BB, BC(R1R 2)B, BCCB, CBC, 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 μMU. Structure-activity relationships (SARs) data for the compounds were investigated and are discussed.
KW - Basement membrane invasion
KW - Gelatinase
KW - Matrix Metallo-proteinase
KW - Organoboronates
KW - Structure-activity relationships
UR - http://www.scopus.com/inward/record.url?scp=3042741361&partnerID=8YFLogxK
U2 - 10.1002/ardp.200300827
DO - 10.1002/ardp.200300827
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C2 - 15065076
AN - SCOPUS:3042741361
SN - 0365-6233
VL - 337
SP - 183
EP - 187
JO - Archiv der Pharmazie
JF - Archiv der Pharmazie
IS - 4
ER -
