肉桂酸衍生物的超声无溶剂法合成及生物活性  

Solvent-free synthesis of cinnamic acid derivatives under ultrasonic irradiation and the biological activity

作　　者：段志芳[1] 付莉[1] 李充璧[1] 

机构地区：[1]肇庆学院生物医药工程中心,广东肇庆526061

出　　处：《化学试剂》2013年第10期933-936,共4页Chemical Reagents

基　　金：广东省科学技术厅基金项目(2011101)

摘　　要：以植物源成分肉桂酸为原料,通过酰氯化,无溶剂条件下采用超声波辐射,与硫氰酸铵反应得到中间体肉桂酰基异硫氰酸酯,不经分离直接与取代酰肼类化合物反应,产物经DMF或DMF/水重结晶得到3个肉桂酰硫脲类衍生物及5个肉桂酰胺基噻二唑类衍生物,经红外、质谱和元素分析确认了新化合物的结构,初步的生物活性测试结果表明N-对硝基苯甲酰氨基-N'-肉桂酰基硫脲对人乳腺癌细胞株MDA-MB-231、胰腺癌细胞株MiaPaCa-2、前列腺癌细胞株PC-3细胞有一定抑制作用。The intermediate cinnamic acyl isothiocyanate was synthesized by acylchlorination of cinnamic acid which is ac- tive ingredient of some natural plants and then thioureation with ammonium thiocyanate under ultrasonic irradiation and solvent-free condition. Then it subsequently reacted with sub- stituted hydrazides under the same condition. Three cinnamic acyl thiourea and five cinnamido thiadiazole derivatives had been obtained by recrystallization using DMF or DMF/H20 as solvent. The biological activity test indicated that the com- pound 5c had certain inhibitory activity against human breast cancer cells MDA-MB-231, human pancreatic cancer ceils MiaPaCa-2 and human prostate cancer ceils PC-3.

关 键 词：肉桂酰硫脲 肉桂酰胺基噻二唑 超声辐射 无溶剂合成 生物活性 

分 类 号：O629.9[理学—有机化学]