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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。
Aim To design and synthesize a series of 2- (E) - (3-methoxy-4-cyclopentyloxyphenylmethylene) cyclopentanone derivatives and screen their antitumor activity in vitro. Methods The target compounds were synthesized and the in vitro antitumor activity of the compounds was screened by using human hepatoma cells (Bel-7402) and human oral cancer cells (KB). Results Five target compounds were synthesized, of which three were not reported in the literature. The structure of the compound was confirmed by IR, 1HNMR, MS and elemental analysis. The results of preliminary screening showed that compound 5 had higher activity and IC50 values of Bel-7402 and KB were 1.62μmol·L-1 and 8.04μmol·L-1, respectively, but lower than that of control drug 5-fluorouracil. Conclusion The Mannich base derivative of 2- (E) - (3-methoxy-4-cyclopentyloxyphenylmethylene) cyclopentanone has certain antitumor activity.