Novel antitumor agent family of 1H-benzo[c,d]indol-2-one with flexible basic side chains: Synthesis and biological evaluation

作者：Yin Hong; Xu Yufang; Qian Xuhong^*

来源：Bioorganic & Medicinal Chemistry, 2007, 15(3): 1356-1362.

DOI：10.1016/j.bmc.2006.11.016

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 IC50 0.428 mu m and 1.69 mu m.

• 出版日期2007-2-1
• 单位华东理工大学