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.

基于Pt的药物（例如顺铂）是用于治疗各种实体恶性肿瘤的一线药物。但是，它们代表了主要问题，例如严重的副作用和耐药性。找出结构-活动关系；在这项研究中，Pt（II）和Pt（IV）与具有相似配体的四（2,2'-dipyridylamine）platinum（IV）（1）和dichloro（2,2'-dipyridylamine）platinum（II）（2合成），测试其在不同肿瘤细胞系上的体外活性，并与顺铂进行比较。尽管对非恶性细胞无毒，但两种标题化合物均显示出对HT-29细胞相当大的杀伤活性。因此，该细胞系可用于进一步研究。细胞周期试验表明，复合物1和2对HT-29细胞诱导的细胞周期停滞机制与顺铂相对相似，且明显不同。此外，细胞凋亡分析表明，晚期细胞凋亡/坏死是三种复合物导致细胞死亡的主要疾病。还对HT-29细胞进行了彗星试验和集落形成试验，结果得到了详尽的讨论。