Synthesis and Biological Evaluation of Heterocyclic Substituted Bis(indolyl)methanes.

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 were tested. 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 anticancer leads.

Synthesis of New Piperazine Substituted Chalcone Sulphonamides as Antibacterial Agents.

BACKGROUND: Infection is a global threat to human health, and there is an urgent need to develop new effective antibacterial drugs to treat bacterial infections. OBJECTIVE: To study the antibacterial activity of piperazine substituted chalcone sulphonamides. MATERIALS AND METHODS: A series of novel piperazine substituted chalcone sulphonamides have been prepared, and in vitro antibacterial activity against Staphylococcus aureus, Bacillus subtilis and Escherichia coli strains were evaluated. RESULTS: The results showed that derivatives 6a, 6c and 6h displayed good antibacterial activity against Bacillus subtilis with MIC values of 4.0-8.0 mg/mL. CONCLUSION: Piperazine substituted chalcone sulphonamides may be used as potential antibacterial agents.