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本世纪60年代末期,Barnett Rosenberg与其合作者发现了顺铂(cis-[PtCl_2(NH_3)_2]的抗癌活性.至今,顺铂作为一种有效的抗癌药物虽已广泛运用于临床,但它有严重的肾毒性和胃肠道反应,引起高音失听等副作用.同时顺铂水溶性低,水溶液不够稳定,缓解期短.为此,人们对铂配合物的抗癌活性与配合物结构关系以及配合物中各个配位基团对活性的影响进行了研究.企望能从具有抗癌活性的铂配合物中,筛选出高效、低毒、水溶性高、稳定性好的抗癌药物.
In the late 1960s, Barnett Rosenberg and his co-workers discovered the anticancer activity of cis- [PtCl_2 (NH_3) _2], and cisplatin has been widely used clinically as a potent anticancer drug to date It has serious nephrotoxicity and gastrointestinal reactions, causing side effects such as treble missing, while cisplatin low water solubility, aqueous solution is not stable enough, the remission period is short.Therefore, the anticancer activity of platinum complexes and complex structure As well as the effect of each coordination group in the complex on the activity.It is hoped that the anticancer drug with high efficiency, low toxicity, high water solubility and good stability can be screened from the platinum complexes with anticancer activity.