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Bioorganic and Medicinal Chemistry Letters 2009-Oct

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.

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Waya S Phutdhawong
Wanwikar Ruensamran
Weerachai Phutdhawong
Thongchai Taechowisan

Keywords

Abstract

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)-alpha, interleukin (IL)-6 and IL-1beta in RAW264.7 cells treated with LPS.

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