含DNA嵌入基团的抗肿瘤铂类配合物研究进展

铂类抗肿瘤药物因其独特的抗肿瘤作用机制、显著的抗肿瘤效果以及抗肿瘤谱广等特点，被广泛应用于临床治疗中。而已上市的铂类药物在治疗过程中出现的不良反应、耐药性和交叉耐药性等缺点限制了其进一步扩大应用。铂类配合物结构中引入DNA嵌入基团，其抗肿瘤作用机制与经典铂类药物不同，在克服经典铂类抗肿瘤药物缺点上具有独到的优势。含DNA嵌入基团的铂类配合物以其所含DNA嵌入基团不同可分为6大类:含吲哚嵌入基团的铂类配合物、含吖啶嵌入基团的铂类配合物、含喹啉嵌入基团的铂类配合物、含萘酰亚胺嵌入基团的铂类配合物、含蒽醌嵌入基团的铂类配合物、含其他类嵌入基团的铂类配合物。本文总结了近几年含DNA嵌入基团铂类配合物的抗肿瘤活性研究进展。

Advances in platinum-intercalators of DNA as antitumor agents

Platinum antitumor drugs are widely used for clinical treatment because of their unique antitumor mechanisms, significant antitumor effects, and broad antitumor spectrum. Yet shortcomings such as toxic side effects, drug resistance and cross-resistance of platinum-based drugs have limited their further application. Platinum-intercalator conjugates possess different antitumor mechanisms from those of classic platinum drugs, and have unique advantages in overcoming the disadvantages of classic platinum antitumor drugs. The platinum-intercalator conjugates can be classified into six categories based on the different DNA-intercalator: platinum-acridine, platinum-quinoline, platinum-indole, platinum-naphthalimides, platinum-anthraquinone and platinum-based antitumor agents containing other types of intercalating groups. This article summarizes the research progress of platinum-based antitumor drugs containing DNA insertion groups in recent years.