AI Article Synopsis
- Prostaglandin E (PGE) is involved in inflammation, making its inhibition an important target for drug development.
- Diarylheptanoids are a type of compound that have shown effectiveness in inhibiting PGE, and this study focuses on synthesizing their analogues.
- One of the leading compounds demonstrated a strong inhibitory effect on PGE with an IC value of 0.56 ng/µL, showing no toxicity up to a high concentration of 10 ng/µL.
Article Abstract
Prostaglandin E (PGE) is a lipid mediator of inflammation and its inhibition has become a popular drug target due to its harmful physiological roles. Diarylheptanoids are one class of compounds that have shown successful inhibition of PGE. This paper reports the synthesis and PGE inhibitory activity of a series of analogues of a naturally occurring diarylheptanoid. The most efficacious compounds were examined for dose-dependent PGE inhibition. Among several promising compounds, the lead candidate exhibited an IC value of 0.56 ng/µL or 1.7 µM with no detectable toxicity at the highest dose of 10 ng/µL.
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| http://dx.doi.org/10.1016/j.bmcl.2017.12.046 | DOI Listing |
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