Novel antitumor agent family of 1H-benzo[c,d]indol-2-one with flexible basic side chains: synthesis and biological evaluation.
Novel antitumor agent family of 1H-benzo[c,d]indol-2-one with flexible basic side chains: synthesis and biological evaluation.
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DOI：
10.1016/j.bmc.2006.11.016
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发表时间：
2007-02
影响因子：
3.5
通讯作者：
H. Yin;Yufang Xu;X. Qian
中科院分区：
文献类型：
--
作者：
H. Yin;Yufang Xu;X. Qian
设计并合成了一系列具有不同胺侧链的单1H-苯并[c，d]吲哚-2-酮和双1H-苯并[c，d]吲哚-2-酮作为新型的DNA嵌入剂，分别评价了芳香生色团和胺侧链对DNA结合性能（如嵌入和静电结合）的贡献。其中，N，N-二甲氨基乙基乙二胺加尾的A3对A549和P388细胞具有选择性的抗肿瘤活性，IC 500分别为0.428 μm和1.69μm。
A series of mono-1H-benzo[c,d]indol-2-one with different amine side chains and bis-1H-benzo[c,d]indol-2-one as novel family of DNA intercalators were designed and synthesized, the contributions of aromatic chromophores and amine side chains for DNA binding properties, for example, intercalation and electrostatic binding, respectively, were evaluated. Among them, A3 tailed with N,N-dimethylamino-ethyl-ethane-1,2-diamine showed selective anti-tumor activities against cell lines A549 and P388 with IC500.428μm and 1.69μm.