title: 3-Arylcoumarins: synthesis and potent anti-inflammatory activity.
abstract: Chronic inflammation is the persistent and excessive immune response and can lead to a variety of diseases. Aiming to discover new compounds with anti-inflammatory activity, we report herein the synthesis and biological evaluation of 3-arylcoumarins. Thirty five 3-arylcoumarins were prepared through Perkin condensation and further acid-promoted hydrolysis if necessary. In lipopolysaccharide-activated mouse macrophage RAW264.7 cells, 6,8-dichloro-3-(2-methoxyphenyl)coumarin (16) and 6-bromo-8-methoxy-3-(3-methoxyphenyl)coumarin (25) exhibited nitric oxide production inhibitory activity with the IC₅₀ values of 8.5 μM and 6.9 μM, respectively, providing a pharmacological potential as anti-inflammatory agents.
authors.forename: Wenchen
authors.initials: W
authors.lastname: Pu
authors.forename: Yuan
authors.initials: Y
authors.lastname: Lin
authors.forename: Jianshuo
authors.initials: J
authors.lastname: Zhang
authors.forename: Fei
authors.initials: F
authors.lastname: Wang
authors.forename: Chun
authors.initials: C
authors.lastname: Wang
authors.forename: Guolin
authors.initials: G
authors.lastname: Zhang
mesh_terms: D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D003374:Coumarins / Q000138:chemical synthesis* / Q000737:chemistry; D006801:Humans; D007249:Inflammation / Q000188:drug therapy*
chemical_list: D000893:Anti-Inflammatory Agents; D003374:Coumarins