Synthesis, DNA binding and topoisomerase inhibition of mononaphthalimide homospermidine derivatives

Zhi Yong Tian Hong Xia Ma Song Qiang Xie Xue Wang Jin Zhao Chao Jie Wang Wen Yuan Gao

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 shu
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 shu

Synthesis, DNA binding and topoisomerase inhibition of mononaphthalimide homospermidine derivatives

  • 基金项目:

    and Henan Natural Science Foundations (Nos.0512001300

    072102330028).

    This work is supported by the National Natural Science Foundation of China (No.20472016)

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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  • 收稿日期:  2007-11-22
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