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KMID : 0043320080310020142
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Archives of Pharmacal Research
2008 Volume.31 No. 2 p.142 ~ p.147
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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
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Yoo Ji-Kang
Kim Bok-Hee
Cho Hoon
Cho Hyun-Suk
Choi Cheol-Hee
Chung Yong-Seog
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Abstract
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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 L 1210 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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KEYWORD
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Naphthoquinone, Cytotoxicity, Antitumor Activity
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