Design and synthesis of novel inhibitors of gelatinase B.
A new method was developed to identify nonpeptidic metalloproteinase inhibitors with novel zinc binding groups. Application of this method to matrix metalloproteinase-9 resulted in the identification of aminomethyl benzimidazole analogue 7a with an IC(50)=13 microM.
Center for New Directions in Organic Synthesis, Department of Chemistry, University of California, Berkeley, CA 94720, USA.
Xueqing
X
Wang
Youngchool
Y
Choe
Charles S
CS
Craik
Jonathan A
JA
Ellman
D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001665:Binding Sites; D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D061965:Matrix Metalloproteinase Inhibitors; D015394:Molecular Structure; D012995:Solubility; D015032:Zinc / Q000378:metabolism
D001562:Benzimidazoles; D004791:Enzyme Inhibitors; D061965:Matrix Metalloproteinase Inhibitors; D015032:Zinc