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Design of MMP-1 inhibitors via SAR transfer and experimental validation
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Design of MMP-1 inhibitors via SAR transfer and experimental validation
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Journal Article
Design of MMP-1 inhibitors via SAR transfer and experimental validation
2022
Overview
New matrix metalloproteinase 1 (MMP-1) inhibitors were predicted using the structure–activity relationship (SAR) transfer method based on a series of analogues of kinesin-like protein 11 (KIF11) inhibitors. Compounds
5
–
7
predicted to be highly potent against MMP-1 were synthesized and tested for MMP-1 inhibitory activity. Among these, compound
6
having a Cl substituent at the R
1
site was found to possess ca. 3.5 times higher inhibitory activity against MMP-1 than the previously reported compound
4
. The observed potency was consistent with the presence of an SAR transfer event between analogous MMP-1 and KIF11 inhibitors. Pharmacophore fitting revealed that the higher inhibitory activity of compound
6
compared to compound
4
against MMP-1 might be due to a halogen bond interaction between the Cl substituent of compound
6
and residue ARG214 of MMP-1.
