乙酰胺基丙酰胺衍生物的合成及抗癌活性研究

Synthesis and Anticancer Activity Evaluation of 2-(4-substituted phenyl) Acetamide Propionyl Acidamide Derivatives

以L-苯丙氨酸或L-色氨酸为基本骨架,甲酯化后与4-取代苯乙酸酰胺化,经水解与2-(1H-咪唑-1-基)乙胺反应得到六个新型2-(4-取代苯乙酰胺基)丙酰胺衍生物5a～5f。化合物结构通过IR、1H NMR和元素分析进行确证。通过MTT法测试了目标化合物对人非小细胞肺癌细胞A-549的抑制活性。初步抗癌活性测试表明,化合物5e具有明显的抑制肿瘤细胞增殖活性。

Six 2 -（4 -substituted phenyl） acetamide propionyl acidamide derivatives （Sa ~5f） were designed and synthesized. They were prepared of L - phenylalanine or L - tryptophan as the basic skeleton by esterification with the methanol, amidation with alphatoluic acid derivatives, then hydrolysis and amidation with 2 - （ 1H - imidazol - 1 - yl） ethanamine. The structures of compounds were confirmed by IR, 1H NMR spectra and elemental analysis. The anticancer activities of the terget compounds were tested on human non - small cell lung cancer cells A -- 549 by MTT assay. The re- suits exhibited that compound 5e had prominence antiproliferative activities by preliminary test.