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与顺二氨合铂(II)络合的硒代嘌呤和硫代嘌呤的合成及抗肿瘤活性

Synthesis and antitumor activity of seleno- and thio-purines complexed with cis-diamminoplatinum (II).

作者信息

Maeda M, Abiko N, Sasaki T

出版信息

J Pharmacobiodyn. 1982 Feb;5(2):81-7. doi: 10.1248/bpb1978.5.81.

Abstract

cis-Diamminoplatinum (II) complexes with selenoguanine, thioguanine, 6-thioxanthine, or 6-mercaptopurine were synthesized by the reaction of stoichiometric amounts of selenopurine or thiopurine with aquated cis-dichlorodimmineplatinum (II) in slightly acidic medium, and their antitumor activity was studied against L1210 cells in mice. These compounds exhibited a medium antitumor activity with very low toxicity. The antitumor activity was dependent on the nature of the purine ligand. These complexes were very stable in various aqueous solvents at 37 degrees C for 10 d but not in the presence of mouse serum. The mechanism of the action effected by the complex is not clear. However, the slow release of an antitumor active purine from the complex, SeG-Pt (NH3)2, was observed.

摘要

通过在微酸性介质中使化学计量的硒嘌呤或硫嘌呤与水合顺式二氯二氨铂(II)反应,合成了顺式二氨铂(II)与硒鸟嘌呤、硫鸟嘌呤、6-硫代黄嘌呤或6-巯基嘌呤的配合物,并研究了它们对小鼠L1210细胞的抗肿瘤活性。这些化合物表现出中等抗肿瘤活性且毒性极低。抗肿瘤活性取决于嘌呤配体的性质。这些配合物在37℃的各种水性溶剂中10天内非常稳定,但在小鼠血清存在下则不然。该配合物的作用机制尚不清楚。然而,观察到抗肿瘤活性嘌呤从配合物SeG-Pt(NH3)2中缓慢释放。

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