Abstract
Dehydroxymethylepoxyquinomicin (DHMEQ, 1) is a novel nuclear factor-κB (NF-κB) inhibitor that inhibits DNA binding of NF-κB components including p65. To inspect its biological activity of 1, we synthesized parasitenone (3), possessing the common epoxycyclohexenone moiety of 1. Assessment of the inhibitory activity against NF-κB indicated that the epoxycyclohexenone moiety is the most essential element for the NF-κB inhibitory activity and the salicylic acid moiety may contribute the binding efficiency and specificity.
| Original language | English |
|---|---|
| Pages (from-to) | 5383-5386 |
| Number of pages | 4 |
| Journal | Bioorganic and Medicinal Chemistry Letters |
| Volume | 19 |
| Issue number | 18 |
| DOIs | |
| Publication status | Published - 2009 Sep 15 |
Keywords
- Anodic oxidation
- DHMEQ
- Epoxycyclohexenone
- NF-κB inhibitor
- Parasitenone
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry
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Saitoh, T., Suzuki, E., Takasugi, A., Obata, R., Ishikawa, Y., Umezawa, K., & Nishiyama, S. (2009). Efficient synthesis of (±)-parasitenone, a novel inhibitor of NF-κB. Bioorganic and Medicinal Chemistry Letters, 19(18), 5383-5386. https://doi.org/10.1016/j.bmcl.2009.07.120