LAUSR

Bis(indolyl)methane derivatives, also considering as metabolites of indole alkaloids, are widely found in nature with a broad range of biological and pharmacological activities. In this work, a series of heterocyclic substituted bis(indolyl)methanes (3a-3p) have been prepared by condensation reaction of indole and heterocyclic aldehydes catalyzed by boron trifluoride etherate with high yields. The structures were characterized by 1H NMR, 13C NMR and HRMS. Preliminary in vitro anti-inflammatory in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and cytotoxic activity against human tumor cell lines (A549, Hela and SGC7901) by MTT assay were tested. The result indicated that bis(indolyl)methanes showed good anti-inflammatory and selective cytotoxic activity. Especially, compounds 3o, 3p and 3q displayed similar inhibitory effect on the generation of NO to positive control dexamethasone, and compound 3q displayed similar selective cytotoxic activity to 5-FU.