4-酰基-5-吡唑酮的二烃基锡配合物的合成、表征及其抗癌活性研究

SYNTHESIS, CHARACTERIZATION AND IN VITRO ANTITUMOR ACTIVITY OF DIORGANOTIN(IV) COMPOUNDS OF 4-ACYL-5-PYRAZOLONE

摘要: 目的　设计合成一系列新型有机锡化合物，通过药理筛选寻找具有抗肿瘤活性的药物并探讨其构效关系。方法　以4-酰基-5-吡唑酮为配体合成有机锡化合物，用元素分析、红外光谱、 ¹H，¹³C，¹¹⁹Sn NMR等方法对得到的化合物作结构表征并利用几种药理模型进行体外抗癌活性筛选。结果　合成了一系列R₂SnL₂ 型有机锡新配合物并确定其结构。结论　药理筛选结果表明，多个化合物(3～6,9～11)对HL-60, HCT-8, Bel-7402,BGC-823和KB癌细胞有效，显示了较强的抗癌活性。

Abstract: AIM　A series of novel diorganotin (IV) compounds had been synthesized in order to find candidates with antitumor activities by in vitro screening. METHODS　The title compounds were prepared using new β-diketonate donors, 4-acyl-5-pyrazolone as ligands. These new compounds were characterized by elemental analyses, IR spectra, ¹H, ¹³C and ¹¹⁹Sn NMR and screened by several antitumor models in vitro. RESULTS　Nine new compounds formulated as R₂SnL₂ (HL is 4-acyl-5-pyrazolone ligand) were synthesized and their structures were determined. CONCLUSION　Several compounds 3～6 and 9～11 showed different inhibitory effects on HL-60, HCT-8, Bel-7402, BGC-823 and KB cells in vitro and are worthy of further study.