目的设计合成一系列全新的查耳酮类衍生物,并初步测试其蛋白酪氨酸激酶(PTKs)抑制活性。方法以间二甲苯为原料,经硝化、还原、水解、甲氧甲基保护等反应得到中间体取代苯乙酮,该中间体再与取代苯甲醛发生羟醛缩合反应后脱保护基得到目标化合物。采用酶联免疫吸附法(ELISA),以金雀异黄素为阳性对照,对目标化合物进行体外PTKs抑制活性检测。结果与结论合成了10个查耳酮衍生物,其中9个是未见报道的新化合物,10个化合物的结构经核磁共振氢谱和质谱确证。化合物6a及新化合物6b、6c和6d对PTKs具有良好的抑制活性。 Aim To design and synthesize a series of new chalcone derivatives and test their protein tyrosine kinase (PTKs) inhibitory activity. Methods Starting from m-xylene, the intermediate substituted acetophenone was obtained through the reaction of nitration, reduction, hydrolysis and methoxymethyl protection. The intermediate was further subjected to aldol condensation reaction with substituted benzaldehyde to deprotected to give the target compound . Enzyme-linked immunosorbent assay (ELISA) was used to detect the inhibitory activity of the target compounds against PTKs in vitro using genistein as positive control. RESULTS AND CONCLUSION Ten chalcone derivatives were synthesized, of which nine were new compounds that were not reported. The structures of 10 compounds were confirmed by 1H NMR and MS. Compound 6a and new compounds 6b, 6c and 6d have good inhibitory activity on PTKs.