3-(3′-甲基-4′-取代苯基-1′,3′-丁二烯基)吲哚类衍生物的合成及其抗癌活性

SYNTHESIS AND ANTICANCER ACTIVITY OF 3-［(3′-METHYL-4′-(SUBSTITUTED PHENYL)-1′,3′-BUTADIENYL］ INDOLE DERIVATIVES

摘要: 目的　研究3-(3′-甲基-4′-取代苯基-1′,3′-丁二烯基)吲哚类衍生物的合成及其抗癌活性。方法　通过亲电取代、羟醛缩合、选择性还原、相转移Wittig反应和水解反应合成目的化合物，利用几种药理模型进行抗癌和抗炎活性筛选。结果　设计合成了11个3-(3′-甲基-4′-取代苯基-1′,3′-丁二烯基)吲哚化合物，均为新化合物。生物活性实验结果表明，化合物8对HL-60，HCT-8和Bel7402癌细胞株有效，且在浓度为10^-5mol·L^-1时，其抗炎抑制率可达100％。结论　化合物8显示了抑癌作用和抗炎活性，值得进一步研究。

Abstract: AIM　To study the synthesis and anticancer activity of 3-［(3′-methyl-4′-(substituted phenyl)-1′,3′-butadienyl］ indole derivatives. METHODS　Electrophilic-substitution, aldol-condensation, selective-reduction, phase-transfer Wittig reaction and hydrolysis reaction were used in the synthesis of the title compounds. RESULTS　Eleven compounds of 3-［(3′-methyl-4′-(substituted phenyl)-1′,3′-butadienyl］ indole were synthesized. They are new compounds. Compound 8 showed different inhibitory effects on HL-60, HCT-8 and Bel7402 cell lines in vitro, and its inhibitory rate of antiinflammation was 100％ at 10^-5 mol·L^-1 concentration. CONCLUSION　Compound 8 showed high anticancer and antiinflammatory activities, and is worth further studying.