Archives of Pharmacal Research
- Volume 22 Issue 5
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- Pages.507-514
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- 1999
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- 0253-6269(pISSN)
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- 1976-3786(eISSN)
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
- Chae, Gyu-Han (College of Pharmacy, Chungnam National University) ;
- Song, Gyu-Yong (College of Pharmacy, Chungnam National UniversitCollege of Pharmacy, Chungnam National University) ;
- Kim, Yong (y) ;
- Cho, Hoon (Kuhnil Pharmaceutical Co.) ;
- Sok, Dai-Eun (College of Pharmacy, Chungnam National University) ;
- Ahn, Byung-Zun (College of Pharmacy, Chungnam National University)
- Published : 1999.10.01
Abstract
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.
Keywords
- Azidoalkylated naphthoquinones;
- DNA topoisomerase-I inhibition;
- Antitumor activity;
- Structure-activity relationship