Background: Bis(indolyl)methane derivatives are widely found in nature with a broad range of
biological and pharmacological activities. The development of techniques for the synthesis and
functionalization of bis(indolyl)methanes have attracted more and more attention in recent years.
Objective: To study the synthesis and biological activity of heterocyclic substituted bis(indolyl)methanes.
Materials and Methods: 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. 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
Results: The result indicated that heterocyclic substituted bis(indolyl)methanes showed good antiinflammatory
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.
Conclusion: Heterocyclic substituted bis(indolyl)methanes may be used as potential anti-inflammatory and