有机锗蒽醌酰胺和有机锗萘酚酯倍半氧化物的合成及对体外培养癌细胞的抑制作用

摘要

Objective To synthesize new organogermanium compounds with stronger cytotoxic activities,and study the relationship between the structure and anticancer activity.Methods Four organogermanium compounds with anthraquinone or naphthalene moiety were synthesized,their structures were determined by IR,1HNMR,and elemental analysis.Their cytotoxicity were evaluated against human chronic myeloid leukemia K562 cell lines.The experiments were repeated three times.Results The antiproliferative effect was assayed by determined the IC50,the drug concentration(μmol/L)required to inhibit cell growth by 50%,and the results were 11.2,16.3,4.8,and 9.3,respectively.The antitumor activity was markedly enhanced relative to that of the reference compounds 2-amino-anthraquinone(IC50 =771μmol/L)and 1-naphtol(IC50 =282μmol/L).Conclusion The cytotoxicity could be improved by the introduction of planar aromatic chromophore moiety to the parent compound,Ge-132.%目的 合成更强抗癌活性的有机锗化合物,研究分子结构和抗癌活性之间的关系.方法 首先合成了 4 种含蒽醌酰胺和萘酯基团的新型有机锗化合物,用IR,1HNMR和元素分析研究它们的结构.用MTT 方法研究化合物对人白血病癌细胞(K562)的抑制作用.结果 4种化合物对K562的IC50 分别为11.2,16.3,4.8,9.3μmol/L.而参照物2-氨基蒽醌和1-萘酚的IC50分别为771和282μmol/L,Ge-132对体外培养细胞几乎没有抑制作用.结论 对Ge-132进行结构修饰,合成的新型有机锗化合物具有抑制体外培养癌细胞增殖的作用.