| 两种新型水溶性庚铂衍生物的合成和抗癌活性研究 | |
| Synthesis and Anti-Tumor Activity of Two New Water-Soluble Derivatives of Heptaplatin | |
| 摘要: 设计、合成出两种新型的水溶性庚铂衍生物cis-（4R，5R）-4，5-双（氨甲基）-2-乙基-1，3-二氧环戊烷·3-羟基-1，1-环丁烷二羧酸根合铂(Ⅱ)和cis-（4R，5R）-4，5-双（氨甲基）-2-甲基-1，3-二氧环戊烷·3-羟基-1，1-环丁烷二羧酸根合铂(Ⅱ)，并采用元素分析、质谱、红外光谱和核磁共振谱表征了它们的化学结构。体内外抗癌试验表明，虽然它们的细胞毒性不如庚铂，但体内抗癌作用优于庚铂，且水溶性明显高于庚铂，值得进一步研究。 | |
| 关键词: 铂类化合物 合成 抗癌活性 | |
| 基金项目: 国家自然科学基金（No.21161010）；国家重大新药创制专项课题（No.2009ZX09103-109）资助项目。 | |
| Abstract: Two water-soluble derivatives of heptaplatin, cis-[(4R,5R)-4,5-bis(aminomethyl)-2-R-1,3-dioxolane](3-hydroxy-1,1-cyclobutanedicarboxylato) platinum(Ⅱ) (R=ethyl and methyl), were synthesized and characterized by elemental analysis, FAB+-MS and FT-IRalong with 13C NMR. They were evaluated for the cytotoxicity against three human cancer cell lines and for the antitumor activity in the murine S180 model. The results show that despite their cytotoxic potency slightly lower than that of heptaplatin, the derivatives exhibits higher antitumor activity and are worthy of further research. | |
| Keywords: platinum complexes synthesis anti-tumor | |
| 投稿时间：2013-06-14 修订日期：2013-08-01 | |
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| 姜婧,楼丽广,谌喜珠,徐永平,叶青松,刘伟平.两种新型水溶性庚铂衍生物的合成和抗癌活性研究[J].无机化学学报,2014,30(2):317-322. | |
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