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自从顺氯氨铂(DDP)应用于临床以来,铂类化合物的抗肿瘤作用越来越受到重视。Tobe发现某些二羟基Ⅳ价铂合物具有较高的水溶性和抗瘤活性。南京大学配位化学研究所合成反式二羟基铂络合物,发现其具有水溶性高、毒性低的特点,我们所动物实验研究证明几种Ⅳ价铂合物对大鼠W-256癌肉瘤有明显的抗瘤作用,发现其中的二羟基丙二酸二氨合铂是Ⅳ价铂化合物中抗瘤作用较好,毒性较小,但其水溶性较差,且用量较大。鉴于二异丙胺合铂类(Ⅱ价)对小鼠白血病L_(1210)有效,南京大学配位化学研究所又合成
Since the application of cisplatin (DDP) to the clinic, the anti-tumor effect of platinum compounds has gained more and more attention. Tobe discovered that certain dihydroxy IV valence platinum compounds have higher water solubility and antitumor activity. The synthesis of trans-dihydroxy-platinum complexes by the Institute of Coordination Chemistry, Nanjing University, has been found to have high water-solubility and low toxicity. Our experimental animal studies have demonstrated that several IV-valent platinum complexes are active against rat W-256 carcinosarcoma. There is a clear anti-tumor effect, found that diammine diammine diammine platinum is a platinum compound with good anti-tumor effect, less toxicity, but its poor water solubility, and a larger amount. Given that diisopropylamine platinum (II) is effective against mouse leukemia L_(1210), the Institute of Coordination Chemistry, Nanjing University has synthesized