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

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(英文)

作　　者：闫星[1] 马玉卓 陈静波[2] 刘鹰翔[1,3] 

机构地区：[1]广东药学院药科学院 [2]云南大学教育部自然资源药物化学重点实验室 [3]广州中医药大学中药学院,广东广州510006

出　　处：《Journal of Chinese Pharmaceutical Sciences》2007年第4期268-271,共4页中国药学（英文版）

基　　金：Natural Science Foundation of GuangdongProvince(Grant No.994615).

摘　　要：Aim To design and synthesize a series of 2-（E）-（4-cyclopentyloxy-3-methoxylbenzylidene）cyclopentanone derivatives, and to determine their antitumor activities in vitro. Method The target compounds were synthesized. Their antitumor activities were assayed using human hepatic carcinoma ceil line （Bel-7402） and human oral cavity epidermis squamoceilular carcinoma 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 better biological activity with IC50 1.62 μmol·L^-1 against Bel-7402 and 8.04 μmol·L^-1 against KB, but much weaker than 5- Fluorouracil. Conclusion Mannich base derivatives of 2-（E）-（4-cyclopentyloxy-3-methoxylbenzylidene）cyclopentanone exhibited some antitumor activities.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、1HNMR、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1.62μmol·L–1和8.04μmol·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。

关 键 词：Chemical synthesis Benzylidenecyclopentanone substituted Antitumor activity 

分 类 号：R914[医药卫生—药物化学] R730.5[医药卫生—药学]