Synthesis and evaluation of antitumor activity of novel 2-[N-Methyl-N-(4-methyl-1,3-benzothiazol-2-yl)aminomethyl]-5,8-diacyloxy-1,4-naphthoquinones

被引：0
作者：
Jikang Yoo
Hyun-Suk Choi
Cheol-Hee Choi
Yongseog Chung
Bok Hee Kim
Hoon Cho
机构：
[1] Chosun University,Department of Polymer Science & Engineering
[2] Chungbuk National University,College of Pharmacy and BK21
[3] Chosun University Medical School,Research Center for Resistant Cells and Department of Pharmacology
[4] Chungbuk National University,Department of Chemistry, Institute for Basic Science, CBITRC
[5] Chosun University,Department of Food Science and Nutrition
来源：
Archives of Pharmacal Research | 2008年 / 31卷
关键词：
Naphthoquinone; Cytotoxicity; Antitumor Activity;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A series of nine new compounds bridged by acyl groups at the 5,8-dihydroxyl group of DHNQ were synthesized and their cytotoxic activity against L1210 and P388 cancer cells was examined. Their antitumor action in mice bearing S-180 cells in the peritoneal cavity was also assessed. Increasing the size of the acyl group (compounds 7–9) up to propyl increased the antitumor activity (T/C value), whereas the cytotoxicity of these compounds was comparable against L1210 (lymphocytic leukemia) and P388 (lymphoid neoplasm) cancer cells. Further increasing in the chain length (compounds 11–15) decreased the potency. Thus, acyl group chains of three carbon atoms is optimal for antitumor activity. The most potent compound of this series was 2-[N-methyl-N-(4-methyl-1,3-benzothiazol-2-yl)aminomethyl]-5,8-dipropylcarbonyloxy-1,4-naphthoquinone (compound 9) with a T/C (%) value of 354.
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页码：142 / 147
页数：5
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