Two new copper(II) complexes, 9-PMAH-Cu (1) and 9-FPMAH-Cu (2), of anthrahydrazone were synthesized and structurally characterized, in which 9-FPMAH is the 4′-CF₃ derivative of 9-PMAH. Both complexes 1 and 2 showed similar intercalative binding modes towards DNA and might compete with the typical DNA intercalator, GelRed, in the same binding site. They could also act as Topo-I suppressor to effectively inhibit its activity, in which complex 1 was more effective than 2. The in vitro antitumor screening indicated that complex 1 displayed much higher antiproliferative ability than 2 and cisplatin towards all the tested tumor cell lines. On the other hand, complex 1 also showed high cytotoxicity against human normal liver cell line HL-7702, suggesting it is a potential high cytotoxic antitumor candidate. While it was also suggested that the loss of activity of complex 2 might be due to the presence of 4′-CF₃ on the pyrimidine ring. Studies on the cellular level showed that complex 1 could arrest the cell cycle of the most sensitive T-24 cells at G2/M phase and induced cell apoptosis. Complex 1 further showed a significant suppression on the tumor growth on the T-24 tumor xenograft mouse model, without apparent losses in their body weight, which suggests that complex 1 is of enough safety to be considered as a promising anticancer candidate by combining the bioactive Cu(II) and the anthrahydrazone pharmacophore. And more anticancer explorations on the copper complexes of anthrahydrazone are intriguing and expected.

合成了腙的两种新的铜(II)配合物9-PMAH-Cu ( 1 ) 和9-FPMAH-Cu ( 2 )，并对其进行了结构表征，其中9-FPMAH是9-的4′-CF ₃衍生物。 PMAH。复合物1和2对 DNA 显示出相似的嵌入结合模式，并可能在相同的结合位点与典型的 DNA 嵌入剂 GelRed 竞争。它们还可以作为 Topo-I 抑制剂来有效抑制其活性，其中复合物1比2更有效。的体外抗肿瘤筛查表明复杂1显示高得多的抗增殖能力比2和顺铂对所有测试的肿瘤细胞系。另一方面，复合物1对人正常肝细胞系 HL-7702 也显示出高细胞毒性，表明它是一种潜在的高细胞毒性抗肿瘤候选物。同时也提出复合物2活性的丧失可能是由于嘧啶环上存在4'-CF ₃。细胞水平的研究表明，复合物1可以在G2/M期阻滞最敏感的T-24细胞的细胞周期并诱导细胞凋亡。复合物1在 T-24 肿瘤异种移植小鼠模型上进一步显示出对肿瘤生长的显着抑制，而其体重没有明显下降，这表明复合物1通过结合生物活性 Cu(II) 和蒽腙药效团，具有足够的安全性，被认为是一种有前途的抗癌候选药物。对蒽腙铜配合物的更多抗癌探索令人感兴趣和期待。