In situ “click” assembly of small molecule matrix metalloprotease inhibitors containing zinc-chelating groups
M Hu, J Li, S Q. Yao - Organic letters, 2008 - ACS Publications
M Hu, J Li, S Q. Yao
Organic letters, 2008•ACS Publications… (3b-3e) Our ongoing research interests in the use of high-throughput amenable chemistry
(such as “click chemistry” and amide-forming reactions) (4) have recently led us to the
development of “click” assembled, hydroxamate-containing peptide analogues which showed
micromolar inhibitory activities against various MMPs. (5) Herein, we describe a “one-pot” click
chemistry procedure for the rapid assembly of small molecule MMP inhibitors containing novel
… We eventually found that D or E (1 equiv) and C1−C28 (1.1 equiv) with K 2 CO 3 (1 equiv; …
(such as “click chemistry” and amide-forming reactions) (4) have recently led us to the
development of “click” assembled, hydroxamate-containing peptide analogues which showed
micromolar inhibitory activities against various MMPs. (5) Herein, we describe a “one-pot” click
chemistry procedure for the rapid assembly of small molecule MMP inhibitors containing novel
… We eventually found that D or E (1 equiv) and C1−C28 (1.1 equiv) with K 2 CO 3 (1 equiv; …
A panel of small molecule-based MMP inhibitors containing rhodanine warheads was assembled using “one-pot” click chemistry. Upon biological screening, moderate inhibitors were identified which specifically targets MMP-7 and MMP-13 over other MMPs.
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