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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。
In this paper, we have synthesized and characterized eight novel platinum complexes containing TMCPDA (TMCPDA = 1,2,2’-trimethyl-1,3-cyclopentanediamine Amine). The inhibitory effects of eight complexes on mouse lymphatic leukemia L-1210 and S-180 sarcoma were determined. The electronic structures of the complexes were also studied. The results show that the series of complexes have higher anticancer activity, especially the inhibitory effect of [Pt (TMCPDA) (Ac-Cl) 2] complex on L-1210 and S-180 is especially in this series of complexes prominent. Further preclinical pharmacological studies have shown that the complex has high activity and low toxicity. The results of electronic structure and anticancer activity of the complexes are in good agreement with the structure-activity relationship of the previously obtained anticancer platinum complexes, indicating that the electronic structure of the complex is indeed closely related to its anticancer activity.