Cytotoxic activity and DNA binding of naphthalimide derivatives with amino acid and dichloroacetamide functionalizations

Ke-Rang Wang Feng Qian Xiao-Man Wang Guan-Hai Tan Rui-Xue Rong Zhi-Ran Cao Hua Chen Ping-Zhu Zhang Xiao-Liu Li

Citation:  Ke-Rang Wang, Feng Qian, Xiao-Man Wang, Guan-Hai Tan, Rui-Xue Rong, Zhi-Ran Cao, Hua Chen, Ping-Zhu Zhang, Xiao-Liu Li. Cytotoxic activity and DNA binding of naphthalimide derivatives with amino acid and dichloroacetamide functionalizations[J]. Chinese Chemical Letters, 2014, 25(7): 1087-1093. doi: 10.1016/j.cclet.2014.04.020 shu

Cytotoxic activity and DNA binding of naphthalimide derivatives with amino acid and dichloroacetamide functionalizations

    通讯作者: Ke-Rang Wang,
    Xiao-Liu Li,
  • 基金项目:

    the Hebei Natural Science Foundation (No. B2012201041)  (No. B2012201041)

    the Foundation of Hebei Education Department (No. YQ2013006). (No. YQ2013006)

摘要: A series of novel naphthalimide derivatives modified by amino acids and their dichloroacetamide derivatives at the 3-position have been synthesized. Their cytotoxic activities were preliminarily evaluated against Hela, A549 and K562 cells, which showed that the length of the side chains of the amino acids influenced the cytotoxic activities. Moreover, compound 7d showed a very good cytotoxic activity against A549 cells with an IC50 value of 4.78 mmol L-1. Furthermore, the UV-vis, fluorescence, and circular dichroism (CD) spectroscopies and thermal denaturation experiment indicated that compounds 6a, 6d and 7a, 7d, as DNA intercalators, exhibited binding affinities with calf-thymus DNA (Ct-DNA).

English

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  • 收稿日期:  2014-03-05
  • 网络出版日期:  2014-04-09
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