| 一些含TMCPDA抗癌铂配合物的研究 |
| STUDY ON SOME ANTITUMOR PLATINUM COMPLEXES WITH TMCPDA |
|
| 摘要: 本文根据大量的抗癌铂配合物的构效关系研究结果,合成及表征了八种含TMCPDA的新铂配合物(TMCPDA=1,2,2'—三甲基—1,3—环戊二胺),测定了八种配合物对小鼠淋巴白血病L—1210及S—180肉瘤的抑制作用,并研究了配合物的电子结构。结果指出,该系列的配合物有较高的抗癌活性,特别是[Pt(TMCPDA)(Ac—Cl)2]配合物对L—1210及S—180的抑制作用在此系列配合物中尤为突出。经进一步的临床前的药理研究表明,该配合物的活性较高、毒性较低。配合物的电子结构与抗癌活性的关系的研究结果与以前所得到的抗癌铂配合物的构效关系较一致,表明配合物的电子结构确实与其抗癌活性密切相关。 |
| 关键词: 抗癌活性 1,2,2′-三甲基-1 3-环戊二胺 铂配合物 小鼠淋巴白血病L-1210 S-180肉瘤 |
| 基金项目: |
| Abstract: On the basis of study on the relationship between the structure and antitumor activity of platinum compounds, eight new platinum complexes of TMCPDA (TMCPDA=1,2,2'-trimethyl-1,3-diaminocyclopentane) were designed, synthesized and characterized, and their electronic structures were studied. The antitumor activity of the compounds against L-1210 Leukemia and S-180 Sarcoma in mice were determined. The results indicate that most of synthesized compounds possess higher antitumor activity. Among them CPt(TMCPDA)(Ac-Cl)2] has superior activity against the ascites Sarcoma 180 tumor, L-1210 Leukemia in mice and are in good agreement with the quantitative relationship between activity and structure of platinum complexes. The obtained results also show, that the compound [Pt(TMCPDA)(Ac-Cl)2 ] just has higher positive charge on Pt atom, more nagative charge on X, lower overlap population on Pt-X, higher Qpt-N medium ΔE values and such electronic characters which are required for a platinum drug with higher activity and lower toxicity as shown by the obtained structure-function relationship previously. |
| Keywords: antitumor activity 1,2,2'-trimethyl-1,3-diaminocyclo-pentane platinum complex L-1210 Leukemia S-180 Sarcoma |
| 投稿时间：1987-09-09 |
| 摘要点击次数: 1420 |
| 全文下载次数: 1146 |
| 曲筠,唐雯霞,戴安邦,籍秀娟,张福荣,刘晓梅.一些含TMCPDA抗癌铂配合物的研究[J].无机化学学报,1988,4(2):90-96. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
| Support information: |
|
|
|
|
|
|
