Pt-based drugs such as cisplatin are frontline drugs used for the treatment of different solid malignancies. However, they represent major problems, such as severe side effects and drug resistance. To find out the structure–activity relationship; in this study, Pt(II) and Pt(IV) complexes with similar ligands, namely tetrachloro(2,2′-dipyridylamine)platinum(IV) (1) and dichloro(2,2′-dipyridylamine)platinum(II) (2) were synthesized, tested for their in vitro activity over different tumor cell lines and compared with cisplatin. Despite nontoxicity against nonmalignant cells, both titled compounds depict considerable killing activity over HT-29 cells. So, this cell line is served for further investigation. Cell cycle test revealed that the mechanism of cell cycle arrest induced by complexes 1 and 2 over HT-29 cells was relatively similar and obviously different from cisplatin. Moreover, apoptosis analysis showed that late apoptosis/necrosis is the primary disease for the death of cell by three complexes. Comet assay and colony-forming test were also performed on HT-29 cells whose results were thoroughly discussed.

顺铂等铂类药物是用于治疗不同实体恶性肿瘤的一线药物。然而，它们也存在一些重大问题，例如严重的副作用和耐药性。找出构效关系；在本研究中，Pt(II) 和 Pt(IV) 具有相似的配体，即四氯(2,2'-二吡啶胺)铂(IV) ( 1 ) 和二氯(2,2'-二吡啶胺)铂(II) ( 2 ) 被合成，测试其对不同肿瘤细胞系的体外活性，并与顺铂进行比较。尽管对非恶性细胞无毒性，但这两种标题化合物都对 HT-29 细胞具有相当大的杀伤活性。因此，该细胞系有待进一步研究。细胞周期测试表明，复合物1和2对HT-29细胞的细胞周期阻滞机制与顺铂较为相似，且明显不同。此外，细胞凋亡分析表明，晚期凋亡/坏死是三种复合物导致细胞死亡的主要原因。还对HT-29细胞进行了彗星实验和集落形成实验，其结果进行了深入讨论。