Inhibitory Activity of Halogenated 3-Benzylidenechroman-4-ones Against Lipopolysaccharide-stimulated Reactive Oxygen Species Production in RAW 264.7 Macrophages

Til Bahadur Thapa Magar, Tara Man Kadayat, Hye Jin Oh, Pil-Hoon Park, Eun-Seok Lee

Chromanone-containing compounds have been reported to possess several important biological activities. As a part of our continuing effort for discovering potent anti-inflammatory agents, a series of halogen-containing 3-benzylidenechroman-4-ones (1–15) were synthesized, and evaluated for their inhibitory effect on lipopolysaccharide (LPS)-stimulated reactive oxygen species (ROS) production in RAW 264.7 macrophages. Compounds 4 and 10 exhibited significant inhibitory activity (IC50  = 5.09 ± 1.27 and 5.11 ± 0.51 μM, respectively) against LPS-stimulated ROS production in RAW 264.7 macrophages.

The LC/MS analysis was carried out using Advion Expression® CMS ESI.