3-(取代苯基乙烯基)吲哚类衍生物的合成及抗肿瘤活性

SYNTHESIS AND ANTITUMOR ACTIVITY OF 3 (SUBSTITUTED PHENYL)VINYL INDOLE DERIVATIVES

摘要: 目的:合成一系列以吲哚为母核,具有第三代维甲类结构特征的化合物(3取代苯基乙烯基吲哚衍生物) ,通过药理筛选寻找具有抗肿瘤活性的物质。方法:通过Wittig 反应、WittigHorner 反应和相转移Wittig 反应得到目的物,利用几种药理模型进行抗肿瘤和免疫活性筛选。结果:设计合成了29 个新的3( 取代苯基乙烯基) 吲哚化合物,药理筛选结果表明,5 个化合物(9,12,13,15,17) 对HCT8, KB和Bel7402 细胞株有效,1 个化合物具有较高的增强免疫活性。结论:药理筛选结果表明,其中一些化合物显示了较强的抗肿瘤和增强免疫活性。

Abstract: AIM: A series of 3 (substituted phenyl)vinyl indole derivatives had been synthesized in order to find compounds with antitumor activity by screening in vitro. METHODS: Title compounds were synthesized by Wittig reaction, Wittig Horner reaction and Phase Transfer Wittig reaction. RESULTS: Twenty nine compounds of 3 (substituted phenyl)vinyl indole were synthesized. Five compounds showed different inhibitory effects on HCT 8 and KB and Bel7402 cell lines in vitro, and one compound high activity on immunity. CONCLUSION: Some compounds with high antitumor and immunoincreasing activities were obtained and is worth while for further study.