新型氨基嘧啶环戊并[b]吲哚衍生物的合成及抗肿瘤活性

Sythesis and Anti-tumor Activities of Novel Aminopyrimidinecyclopenta[b]oxindole Derivatives

以3-吲哚丙酸为原料,经环化、N-甲基化、Claisen-Schmidt缩合和环加成反应合成了新型氨基嘧啶环戊并[b]吲哚衍生物,其结构经1 H NMR、13 C NMR及HR-MS(ESI)表征。采用细胞增殖抑制实验法(MTT法)测定了6a^6j对人肝癌(HepG-2)、人子宫颈癌(Hela)和人鼻咽癌(CNE-1)瘤株的体外抑制活性。结果表明:6b的抑制活性最好,IC 50值分别为大于50μmol/L(HepG-2)、15.2μmol/L(Hela)和14.8μmol/L(CNE-1)。

Using 3-indolepropionic acid as a raw material,ten novel aminopyrimidinecyclopenta[b]indole derivatives were obtained by series of reactions including cyclization,N-methylation,Claisen-Schmidt condensation and cycloaddition.The structures were characterized by 1 H NMR,13 C NMR,and HR-MS(ESI).In addition,the cell proliferation inhibition assay(MTT method)was used to study the in vitro inhibitory activities of 6a^6j on human hepatocelluar carcinomas(HepG-2),human cervical cancer(Hela)and human nasopharyngeal carcinoma(CNE-1)tumor strain.The proliferation inhibition of compound 6a was stronger than others whereas weaker than cisplatin,the proliferation inhibition of 6a were>50μmol/L(HepG-2),15.2μmol/L(Hela)and 14.8μmol/L(CNE-1).