摘要
铂类抗肿瘤药物因其独特的抗肿瘤机制、广泛的抗肿瘤谱、良好的抗肿瘤效果成为目前临床治疗恶性肿瘤最为有效的药物之一.但目前上市的铂类抗肿瘤药物都属于经典的顺铂类药物,由于其结构的相似性,使得其在临床应用中不可避免地出现了顺式铂类药物的毒副作用和耐药性等问题.双核铂类药物是一类新型的非经典铂类抗肿瘤药物,它的设计突破了经典顺铂类药物的构效关系,其作用机制不同于经典铂类药物,不易产生耐药性,因此受到广泛的关注.本文以桥连基团的不同将其归纳分类,主要有三大类:以多胺为桥连基团的双核铂配合物,以氨基酸或二羧酸为桥连基团的双核铂配合物,以卤素离子为桥连基团的双核铂配合物.
Currently,platinum-based anticancer drugs have become one of the most effective drugs for clinical treatment of malignant tumors due to its unique mechanism of action,a broad range of anticancer spectrum and high activity. However,these platinum-based antitumor drugs have similar structures and display the same side effects and resistance. Dinuclear platinum complexes represent a novel class of non-classical platinum-based antitumor drugs with pharmacological profiles,which are different from mononuclear platinum antitumor drugs used currently. It is believed that dinuclear platinum complexes have the potential to overcome the problem of resistance. Thereby,much attention has been focused on the design of dinuclear platinum-based complexes. The research status of dinuclear anticancer platinum complexes is reviewed. Dinuclear platinum complexes are divided to three types,based on the different linking ligands,namely,alkyl polyamines and their derivatives,amino acid or carboxylates,and haloid anions.
出处
《昆明理工大学学报(自然科学版)》
CAS
2017年第2期51-62,共12页
Journal of Kunming University of Science and Technology(Natural Science)
基金
国家自然科学基金项目(21361014,21302074)
关键词
双核铂配合物
抗肿瘤药物
桥连基团
研究进展
dinuclear platinum complex
antitumor drug
linking ligand
research progress