57027-76-6Relevant articles and documents
Synthesis and PGE2 inhibitory activity of novel diarylheptanoids
McLane, Richard D.,Le Cozannet-Laidin, Léon,Boyle, Maxwell S.,Lanzillotta, Lindsey,Taylor, Zachary L.,Anthony, Sarah R.,Tranter, Michael,Onorato, Amber J.
supporting information, p. 334 - 338 (2018/02/15)
Prostaglandin E2 (PGE2) 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 PGE2. This paper reports the synthesis and PGE2 inhibitory activity of a series of analogues of a naturally occurring diarylheptanoid. The most efficacious compounds were examined for dose-dependent PGE2 inhibition. Among several promising compounds, the lead candidate exhibited an IC50 value of 0.56 ng/μL or 1.7 μM with no detectable toxicity at the highest dose of 10 ng/μL.
Tandem phenolic oxidative amidation-intramolecular diels-alder reaction: An approach to the himandrine core
Liang, Huan,Ciufolini, Marco A.
supporting information; experimental part, p. 1760 - 1763 (2010/10/21)
An oxidative cyclization of dienic sulfonamides mediated by iodobenzene diacetate in TFA, followed by a tandem intramolecular Diels-Alder reaction, achieves desymmetrization of a "locally symmetrical" dienone with good levels of diastereoselectivity and leads to valuable synthetic intermediates for the himandrine alkaloids.