| Synthesis,DNA binding and topoisomerase inhibition of mononaphthalimide homospermidine derivatives |
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| 作者姓名： | Zhi Yong Tian
Hong Xia Ma Song Qiang Xie Xue Wang Jin Zhao Chao Jie Wang Wen Yuan Gao |
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| 作者单位： | a School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China;b Institute of Natural Products & Medicinal Chemistry, Henan University, Kaifeng 475001, China;c Chemistry Department, Henan University, Kaifeng 475001, China |
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| 基金项目： | 国家自然科学基金，河南省自然科学基金 |
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| 摘 要： | Two novel mononaphthalimide homospermidine derivatives （2a, 2b） with three or four methylene unit as linkages were synthesized and evaluated for cytotoxicity against human leukemia K562, murine melanoma B 16 and Chinese hamster ovary CHO cell lines. The presence of homospermidine motif could greatly elevate the potency of 1,8-naphthalimide. Conjugate 2b with longer spacer exhibited higher in vitro cytotoxicity than 2a. The DNA binding experiments indicated that conjugates 2b could bind to herring sperm DNA. The topoisomerase Ⅱ poison trials revealed that 2b could inhibit the activity of top. Ⅱ.
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| 关 键 词： | 共轭聚胺 合成 生物评估 DNA粘合物 单萘二甲酰亚氨衍生物 |
| 修稿时间： | 2007年11月22 |
Synthesis, DNA binding and topoisomerase inhibition of mononaphthalimide homospermidine derivatives |
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| Zhi Yong Tian, Hong Xia Ma, Song Qiang Xie, Xue Wang, Jin Zhao, Chao Jie Wang,Wen Yuan Gao,.Synthesis,DNA binding and topoisomerase inhibition of mononaphthalimide homospermidine derivatives[J].Chinese Chemical Letters,2008,19(5):509-512. |
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| Authors: | Zhi Yong Tian Hong Xia Ma Song Qiang Xie Xue Wang Jin Zhao Chao Jie Wang Wen Yuan Gao |
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| Institution: | a School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China;b Institute of Natural Products & Medicinal Chemistry, Henan University, Kaifeng 475001, China;c Chemistry Department, Henan University, Kaifeng 475001, China |
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| Abstract: | Two novel mononaphthalimide homospermidine derivatives (2a, 2b) with three or four methylene unit as linkages weresynthesized and evaluated for cytotoxicity against human leukemia K562, murine melanoma B 16 and Chinese hamster ovary CHOcell lines. The presence of homospermidine motif could greatly elevate the potency of 1,8-naphthalimide. Conjugate 2b with longerspacer exhibited higher in vitro cytotoxicity than 2a. The DNA binding experiments indicated that conjugates 2b could bind toherring sperm DNA. The topoisomerase Ⅱ poison trials revealed that 2b could inhibit the activity of top. Ⅱ.2008 Chao Jie Wang. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved. |
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| Keywords: | Polyamine conjugate Synthesis Bioevalution |
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