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首页> 外文期刊>RSC Advances >Synthesis, cytotoxic evaluation and DNA binding study of 9-fluoro-6H-indolo[2,3-b]quinoxaline derivatives
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Synthesis, cytotoxic evaluation and DNA binding study of 9-fluoro-6H-indolo[2,3-b]quinoxaline derivatives

机译：9-氟-6H- Indolo [2,3-B]喹喔啉衍生物的合成，细胞毒性评价和DNA结合研究

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摘要

A series of novel 9-fluoro-6H-indolo[2,3-b] quinoxaline derivatives as antitumor agents were synthesized and studied. The designed compounds feature positive charges both at the 11-N position of the aromatic scaffold and the side-chain alkylamino group. The corresponding in vitro antitumor activities were evaluated against MCF-7, HeLa and A549 cancer cell lines and the DNA binding properties of these compounds were characterized by UV-vis, fluorescence, and circular dichroism (CD) spectroscopy as well as thermal denaturation. The obtained results indicate that the dicationic quaternary ammonium salt derivatives of 9-fluoro-6H-indolo[2,3-b] quinoxaline may serve as intercalators with increased DNA binding affinity. Furthermore, both the incorporation of fluorine, and alkyl amino side chains and the introduction of a positive charge at the 11-N position of the aromatic scaffold was shown to be responsible for their antitumor activity and improved DNA binding ability. Taken in concert, these findings may be valuable in the understanding of the antitumor effect of these compounds and may further provide important information for the future optimization of the DNA binding properties of this drug type.
机译：合成并研究了一系列新的9-氟-6H- Indolo [2,3-B]喹喔啉衍生物作为抗肿瘤剂。所设计的化合物在芳族支架和侧链烷基氨基的11-N位置具有正电荷。对MCF-7，Hela和A549癌细胞系评价相应的体外抗肿瘤活性，并且通过UV-Vis，荧光和圆形二色性（CD）光谱以及热变性，表征这些化合物的DNA结合性能。所得结果表明，9-氟-6H- Indolo [2,3-B]喹喔啉的直接季铵盐衍生物可用作具有增加的DNA结合亲和力的嵌入剂。此外，氟和烷基氨基侧链的掺入和烷基氨基侧链和在芳族支架的11-n位置引入正电荷，其负责它们的抗肿瘤活性和改善的DNA结合能力。在音乐会中采取，这些发现可能在理解这些化合物的抗肿瘤效果方面是有价值的，并且可以进一步提供该药物DNA结合性能的未来优化的重要信息。

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  • 来源
    《RSC Advances》 |2017年第66期|共11页
  • 作者

    Gu Zhenyu; Li Yanci; Ma Songliang; Li Shenghui; Zhou Guoqiang; Ding Shan; Zhang Jinchao; Wang Shuxiang; Zhou Chuanqi;

  • 作者单位

    Hebei Univ Coll Chem &

    Environm Sci Key Lab Chem Biol Hebei Prov Key Lab Med Chem &

    Mol Diag Minist Educ Baoding 071002 Peoples R China;

    Hebei Univ Coll Chem &

    Environm Sci Key Lab Chem Biol Hebei Prov Key Lab Med Chem &

    Mol Diag Minist Educ Baoding 071002 Peoples R China;

    Hebei Univ Coll Chem &

    Environm Sci Key Lab Chem Biol Hebei Prov Key Lab Med Chem &

    Mol Diag Minist Educ Baoding 071002 Peoples R China;

    Hebei Univ Coll Chem &

    Environm Sci Key Lab Chem Biol Hebei Prov Key Lab Med Chem &

    Mol Diag Minist Educ Baoding 071002 Peoples R China;

    Hebei Univ Coll Chem &

    Environm Sci Key Lab Chem Biol Hebei Prov Key Lab Med Chem &

    Mol Diag Minist Educ Baoding 071002 Peoples R China;

    Hebei Univ Coll Chem &

    Environm Sci Key Lab Chem Biol Hebei Prov Key Lab Med Chem &

    Mol Diag Minist Educ Baoding 071002 Peoples R China;

    Hebei Univ Coll Chem &

    Environm Sci Key Lab Chem Biol Hebei Prov Key Lab Med Chem &

    Mol Diag Minist Educ Baoding 071002 Peoples R China;

    Hebei Univ Coll Chem &

    Environm Sci Key Lab Chem Biol Hebei Prov Key Lab Med Chem &

    Mol Diag Minist Educ Baoding 071002 Peoples R China;

    Hebei Univ Coll Chem &

    Environm Sci Key Lab Chem Biol Hebei Prov Key Lab Med Chem &

    Mol Diag Minist Educ Baoding 071002 Peoples R China;

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  • 正文语种 eng
  • 中图分类 化学;
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