Rapid assembly of matrix metalloprotease inhibitors using click chemistry
Organic letters, 2006•ACS Publications
A panel of 96 metalloprotease inhibitors was assembled using “click chemistry” by reacting
eight zinc-binding hydroxamate warheads with 12 azide building blocks. Screens of the
bidentate compounds against representative metalloproteases provided discerning
inhibition fingerprints, revealing compounds with low micromolar potency against MMP-7.
The relative ease and convenience of the strategy in constructing focused chemical libraries
for rapid in situ screening of MMPs is thereby demonstrated.
eight zinc-binding hydroxamate warheads with 12 azide building blocks. Screens of the
bidentate compounds against representative metalloproteases provided discerning
inhibition fingerprints, revealing compounds with low micromolar potency against MMP-7.
The relative ease and convenience of the strategy in constructing focused chemical libraries
for rapid in situ screening of MMPs is thereby demonstrated.
A panel of 96 metalloprotease inhibitors was assembled using “click chemistry” by reacting eight zinc-binding hydroxamate warheads with 12 azide building blocks. Screens of the bidentate compounds against representative metalloproteases provided discerning inhibition fingerprints, revealing compounds with low micromolar potency against MMP-7. The relative ease and convenience of the strategy in constructing focused chemical libraries for rapid in situ screening of MMPs is thereby demonstrated.
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