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.
出处
《化学试剂》
CAS
CSCD
北大核心
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)
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
cinnamic acyl thiourea
cinnamido thiadiazole
ultrasonic irradiation
solvent-free synthesis
biological activity
