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合成了10个新的铂络合物和5个已知的铂络合物,对6个铂络合物进行了小鼠S_(180)肉瘤的抗肿瘤活性试验,结果表明:6个铂络合物在所用剂量条件下均有较高的抗肿瘤活性,其抑瘤率T/C为15％至35%,与母体化合物顺铂比较,水溶性较高,毒性较低。适当改变铂络合物的化学结构,在其中引入某些亲水性基团,有利于铂络合物水溶性增加,毒性降低,并保持较高的抗肿瘤活性。
Ten new platinum complexes and five known platinum complexes were synthesized. The anti-tumor activity of six platinum complexes on mouse S 180 sarcoma was tested. The results showed that six platinum complexes The antitumor activity of all the compounds at the dosage was high, and the tumor inhibition rate T / C was 15% -35%. Compared with the parent compound cisplatin, the compound had higher water solubility and lower toxicity. Proper changes in the chemical structure of platinum complexes, in which the introduction of some hydrophilic groups, is conducive to the increase of water solubility of platinum complexes, reduce toxicity, and maintain high anti-tumor activity.