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KMID : 0614020040190010001
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Journal of Pharmaceutical Sciences (C.N.U.)
2004 Volume.19 No. 1 p.1 ~ p.8
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Study on the antitumor activity of 2-propylthio-5,8-dimethoxy-1,4-naphthoquinone
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Song Gyu-Yong
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Abstract
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In a continuation of the search for novel antitumor agent, 5,8-dimethoxy-1,4-naphthoquinone was selected as a lead compound and 2-alkylthio-5,8-dimethoxy-1,4-naphthoquinone derivatives were synthesized from 1,5-dihydroxynaphthalene in 5 steps. Among them, 2-propylthio-5,8-dimethoxy-1,4-naphthoquinone (2-PropylthioDMNQ) exhibited the strongest cytotoxicity (ED_(50), 2.02±0.89 and 9.44±199 μM) against L1210 and A549 cells, respectively. Also, 2-propylthioDMNQ (6C) strongly inhibited adhesion of B16-BL6 cells to gelatin and matrigel coated matrices and exhibited anti-invasive effect of B16-BL6 cells. The T/C value of 2-propylthioDMNQ (6c) treated group was 123±2.65 % in S-180 bearing ICR mice.
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KEYWORD
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2-Propylthio-5, 8-dimethoxy-1, 4-naphthoquinone, cytotoxicity, anti-invasive effect, anti-adhesion effect, T/C value
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