引用本文:
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.
doi:
10.1016/j.cclet.2008.03.006
Citation: 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. doi: 10.1016/j.cclet.2008.03.006

Citation: 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. doi: 10.1016/j.cclet.2008.03.006

Synthesis, DNA binding and topoisomerase inhibition of mononaphthalimide homospermidine derivatives
摘要:
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.
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关键词:
- Polyamine conjugate
- / Synthesis
- / Bioevalution
English
Synthesis, DNA binding and topoisomerase inhibition of mononaphthalimide homospermidine derivatives
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.
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Key words:
- Polyamine conjugate
- / Synthesis
- / Bioevalution

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