Abstract
A series of novel hybrid compounds between benzofuran and N-aryl piperazine have been synthesized and screened in vitro for anti-inflammatory activity in lipopolysaccharide (LPS)-stimulated RAW-264.7 macrophages and for anticancer activity against three human tumor cell lines. The results demonstrated that derivative 16 not only had inhibitory effect on the generation of NO (IC50 = 5.28 μM), but also showed satisfactory and selective cytotoxic activity against human lung cancer line (A549) and gastric cancer cell (SGC7901) (IC50 = 0.12 μM and 2.75 μM, respectively), which was identified as the most potent anti-inflammatory and anti-tumor agent in this study.
Highlights
Natural and synthetic benzofuran derivatives are a class of important organic compounds with a broad range of biological activities, such as antioxidant, anti-inflammatory, antibacterial, antitumor, and so on [1–11]
Nitrogen heterocycles are an important class of compounds having versatile biological activities, which are used in drug design and synthesis, generally as active units [16,17]
Piperazine—one of the most biological active moieties—represents a series of important organic compounds that make up the core structures in medicines and have been widely used in the development of drug molecular design [18,19]
Summary
Natural and synthetic benzofuran derivatives are a class of important organic compounds with a broad range of biological activities, such as antioxidant, anti-inflammatory, antibacterial, antitumor, and so on [1–11]. 2-benzoylbenzofuran compounds have been identified to show potent cytotoxic activities, as exemplified in Scheme 1. 2-benzoylphenyl benzofuran compound (A) [12] and 2-(2,4-dimethoxybenzoyl)-phenyl benzofuran derivative (B) [13] showed potent anticancer activities. 2-(4-imidazoyl benzoyl)benzofuran (D) [15] were attractive with excellent anti-inflammatory and cytotoxic activities (Scheme 1). Nitrogen heterocycles are an important class of compounds having versatile biological activities, which are used in drug design and synthesis, generally as active units [16,17]. Piperazine—one of the most biological active moieties—represents a series of important organic compounds that make up the core structures in medicines and have been widely used in the development of drug molecular design [18,19]
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