The journal editors have selected a recent paper in Chemistry–A European Journal from Philip Chan’s group as a Hot Paper. The work describes a synthetic method to prepare 3a,6-methanoisoindole esters by gold(I)-catalyzed tandem 1,2-acyloxy migration/Nazarov cyclization and Diels-Alder reaction of 1,4,9-dienyne esters. One example was found to inhibit binding of tumor necrosis factor-a (TNF-a) to the tumor necrosis factor receptor 1 (TNFR1) site and TNF-induced nuclear factor k-light-chain-enhancer of activated B cells (NF-kB) activation in cell at a half-maximal inhibitory concentration (IC₅₀) value of 6.6 mM. The study showed the isoindolyl derivative to exhibit low toxicity toward human hepatocellular liver carcinoma (HepG2) cells and its possible mode of activity based on molecular modeling analysis.

The full article is available online at http://onlinelibrary.wiley.com/journal/10.1002/(ISSN)1521-3765/homepage/2111_hotpaper.html