摘要
以穿心莲内酯为先导化合物,在其3-位和19-位进行结构修饰,设计并合成了8个新型的穿心莲内酯环磷酸酯类衍生物(3a^3h),其结构经FT-IR和ESI-MS表征。用MTT法研究了3a^3h的体外抗肿瘤活性。结果表明:11,12-脱水(-1-对甲氧基苯酚)-3,19-环磷酸酯穿心莲内酯(3g)对舌癌细胞(Tca-8113)的抑制作用最强,用药量为1.0×10-4mol·L-1时,3g的抑制率为35.16%。
Eight novel andrographolide cyclophosphate derivatives（3a - 3h） were designed and synthesized by structure-modification on 3- and 19-position of andrographolide, using andrographolide as leading compound. The structures were characterized by FT-IR and ESI-MS. The in vitro antitumor activities of 3a - 3h against human tongue cancer cell（ Tea-8113 ） were investigated by MTT method. The results showed that 3,19- （ p-methoxyphenol ） diolcyclophosphoric -14 -deoxy11,12-didehydroandrographlide（3g） exhibited best antitumor activity. The inhibition rate of 3g was 35.16% with dosage of 1.0 × 10^-4mol · L^-1.
出处
《合成化学》
CAS
CSCD
2015年第9期828-830,共3页
Chinese Journal of Synthetic Chemistry
基金
江西省自然科学基金资助项目(20122BAB205033)
江西省科技支撑计划(20121BBG70013)
关键词
穿心莲内酯
环磷酸酯
结构修饰
合成
抗肿瘤活性
andrographolide
cyclophosphate
structure-modification
synthesis
antitumor activity
