三氮杂十环及其铂(II)配合物的合成以及抗肿瘤活性

Synthesis and antitumor activities of triazacyclodecane and its platinum (II) complex

摘要: 为了寻找具有优良高效低毒的抗肿瘤药物，合成了一种新的1,4,7-三氮杂十环配体及其铂(II)配合物，并经元素分析、 IR、 ¹H NMR、 ¹³C NMR、 MS谱、差热分析和电导方法表征。体外生物活性表明这些化合物具有较强的抗肿瘤活性；用抑瘤率和相对生长率测定了人肝瘤(CA)的抑制作用，体内试验显示铂(II)配合物(C)具有抗人肝癌瘤(CA)作用。其中剂量为12 mg·kg^-1抗瘤活性与对照药相当，它的半数致死量为853.6 mg·kg^-1。

Abstract: To search for potential antitumor drugs with potent efficiency and low toxicity, a novel 1,4,7-triazacyclodecane and its platinum (II) complex were synthesized. These compounds were characterized by elemental analysis, IR, ¹H NMR, ¹³C NMR, MS spectra, thermoanalysis and conductivity measurement. Antitumor activity study indicated these compounds had strong antitumor activity in vitro to some extent. Inhibition of human liver tumor of CA was examined by antitumor rate and growth rate, complex C showed inhibition activity on transplanting-tumor growth of CA, 12 mg·kg^-1 was as potent as cisplatin, its ID₅₀ was 853.6 mg·kg^-1.