Synthesis of indolyl-3-acetonitrile derivatives and their inhibitory effects on nitric oxide and PGE2 productions in LPS-induced RAW 264.7 cells |
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Authors: | Tae Hoon Kwon Ik Hwan Yoon Ji-Sun Shin Young Hun Lee Bong Jin Kwon Kyung-Tae Lee Yong Sup Lee |
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Affiliation: | 1. Department of Life and Nanopharmaceutical Sciences, Kyung Hee University, Seoul 130-701, Republic of Korea;2. Department of Pharmacy, College of Pharmacy, Kyung Hee University, Republic of Korea |
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Abstract: | Arvelexin is one of major constituents of Brassica rapa that exerts anti-inflammatory activities. Several indolyl-3-acetonitrile derivatives were synthesized as arvelexin analogs and evaluated for their abilities to inhibit NO and PGE2 productions in LPS-induced RAW 264.7 cells. Of the indolyl-3-acetonitriles synthesized, compound 2k, which possesses a hydroxyl group at C-7 position of the indole ring and an N-methyl substituent, more potently inhibited NO and PGE2 productions and was less cytotoxic than arvelexin on macrophage cells. |
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Keywords: | Arvelexin Indole-3-acetonitrile Nitric oxide Anti-inflammatory |
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