2-（E）-（3-甲氧基-4-环戊氧基苯基亚甲基）环戊酮衍生物的合成及抗肿瘤活性

目的设计并合成一系列2-（E）-（3-甲氧基-4-环戊氧基苯基亚甲基）环戊酮衍生物，并对其体外抗肿瘤活性进行筛选。方法合成目标化合物并用人肝癌细胞（Bel-7402）和人口腔癌细胞（KB）对化合物的体外抗肿瘤活性进行筛选。结果合成了5个目标化合物，其中3个未见文献报道。化合物的结构经IR、^1H NMR、MS和元素分析确证。初筛结果显示化合物5具有较高的活性，对Bel-7402和KB细胞的IC50值分别为1．62gmol·L^-1和8．04gmol·L^-1,但低于对照药5-氟脲嘧啶。结论2-（E）-（3-甲氧基-4-环戊氧基苯基亚甲基）环戊酮Mannich碱衍生物具有一定抗肿瘤活性。

Synthesis and antitumor activities of 2-(E)-(4-cyclopentyloxy-3-methoxylbenzylidene) cyclopentanone derivatives

Aim To design and synthesize a series of 2-(E)-(4-cyclopentyloxy-3-methoxylbenzylidene)cyclopentanone derivatives,and to determine their antitumor activities fn vitro.Method The target compounds were synthesized.Thek antitumor activities were assayed using human hepatic carcinoma cell line (Bel-7402)and human oral cavity epidermis squamocellular careinoma cell line(KB).Results Five compounds were obtained.Three of them were not reported in the literature and their chemical structures were confirmed by IR 1H NMR,MS and elemental analysis.Preliminary screening results showed that compound 5 possessed Fluorouracil.Conclusion Mannich base derivatives of 2-(E)-(4-eyclopentyloxy-3-methoxylbenzylidene)cyclopcntanone exhibited some antitumor activities.