KMID : 0043319990220050507
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Archives of Pharmacal Research 1999 Volume.22 No. 5 p.507 ~ p.514
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2- or 6-(1-Azidoalkyl)-5,8-Dimethoxy-1,4-Napyhthoquinone: Synthesis, Evaluation of Cytotoxic Activity, Antitumor Activity and Inhibitory Effect on DNA Topoisomerase-I
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Chae Gyu-Han
Song Gyu-Yong Kim Yong Cho Hoon Sok Dai-Eun Ahn Byung-Zun
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Abstract
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6-(1-azidoalkyl)-DMNQ derivatives compared to 2-(1-azidoalkyl)-DMNQ isomers, exhibited higher cytotoxic activity against L1210 mouse leukemia cells and stronger inhibition of DNA topoisomerase-I (TOPO-I), suggesting involvement of steric hindrance. However, similar antitumor activity against mice bearing S-180 cell was shown by 2-an 6-(1-azidoalkyl)-DMNQ derivatives.
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KEYWORD
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Azidoalkylated naphthoquinones, DNA topoisomerase-I inhibition, Antitumor activity, Structure-activity relationship
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