Premium
Matrix Metallo‐Proteinase (MMP‐2) Organoboronate Inhibitors
Author(s) -
Ali Hijazi Abu,
Berkovitz Ronny,
Reich Reuven,
Srebnik Morris
Publication year - 2004
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.200300827
Subject(s) - chemistry , matrix metalloproteinase , in vitro , stereochemistry , enzyme inhibitor , structure–activity relationship , matrix (chemical analysis) , biochemistry , chromatography
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 μM. Structure activity relationships (SARs) data for the compounds were investigated and are discussed.