Synthesis of 1,6,7,8-tetrahydro-naphtho[2,3- d]-azepino[4,5- b]indole-9,14-diones and their inhibitory effects on pro-inflammatory cytokines

The synthesis and inhibitory effects on pro-inflammatory cytokines of 1,5,6,7,8,14b-hexahydro-naphtho[2,3- d]-azepino[4,5- b]indole-9,14-diones are reported. A rapid route to a series of naphthoquinone-fused indole derivatives via irradiation in a modified commercial domestic microwave is reported. The desired products were produced in high yields and short reaction times. The naphthoquinone-fused indole derivatives were evaluated for their pro-inflammatory cytokines responses using lipopolysaccharide (LPS)-stimulated RAW264.7 murine macrophages. The results showed that most of the tested compounds inhibit the production of nitric oxide (NO), prostaglandin (PG)E 2, tumour necrosis factor (TNF)-α, interleukin (IL)-6 and IL-1β in RAW264.7 cells treated with LPS.