中文摘要：

以2-吲哚酮与3,5-二氯嘧啶甲醛为原料,经Knoevenagel加成消除反应和取代反应合成了11个新型的嘧啶拼接3-烯键氧化吲哚衍生物（3a-3k）,产率70%-91%,Z/E值15∶1-〉20∶1,其结构经1H NMR,13C NMR和HR-MS（ESI-TOF）表征。采用MTT法研究了3a-3k对人肺癌细胞（A549）和人白血病细胞（K562）的体外抗肿瘤活性。结果表明：3a,3c,3f,3g和3j对K562具有较好的抑制活性（IC50分别为29.3,27.6,28.5,24.0和27.0μmol·L^-1）,3a,3h和3j对A549具有较好的抑制活性（IC50分别为28.1,16.4和25.2μmol·L^-1）。

英文摘要：

Eleven novel pyrimidine-fused 3-alkenyloxindoles（3a - 3k） were synthesized via a Knoevenagel condensation/substitution reaction of pyrimidine aldehydes with 2-oxindoles. The yields and Z/E of 3a - 3k were 65% - 87% and 5 ∶ 1 - 20 ∶ 1,respectively. The structures were characterized by1 H NMR,13 C NMR and HR-MS（ESI-TOF）. The in vitro antitumor activities against human lung cancer cells（A549） and human leukemia cells（K562） were demonstrated by MTT assays. The results showed that 3a,3c,3f,3g and 3j exhibited good inhibition activities against K562 with IC50 of 29. 3,27. 6,28. 5,24. 0,27. 0 μmol·L^-1,respectively. 3a,3h and 3j exhibited good inhibition acitvities against A549,showing IC50 of 28. 1,16. 4,25. 2 μmol·L^-1,respectively.