天津科技大学学报2017，Vol.32Issue(3)：11-15,5.DOI:10.13364/j.issn.1672-6510.20160317
抗肿瘤Dipodazine及其衍生物的合成与活性
Synthesis and in vitro Cytotoxicity Evaluation of Dipodazine Derivatives as Anticancer Agents
摘要
Abstract
A series of Dipodazine derivatives were synthesized via the amino protecting,electrophilic substitution,hydroxyl aldehyde condensation,and deprotection reaction.Eight derivatives were designed and synthesized in 10%~30% overall yield.The anticancer activity of these new Dipodazine derivatives against three human tumor cell lines,K562,HepG2 and HT-29,were evaluated by MTT assay in vitro.SAR studies suggested that C-5 substitution has great influence on the activ-ity,whereas an amino functionality on N-1 as present in the parent ring is required to such potency.关键词
环二肽/二酮哌嗪/吲哚/抗肿瘤Key words
cyclic dipeptide/2/5-diketopiperazine/indole/antitumor分类
医药卫生引用本文复制引用
孙华,张亚洲,王鹏飞,王栋,张倩,袁媛,滕玉鸥..抗肿瘤Dipodazine及其衍生物的合成与活性[J].天津科技大学学报,2017,32(3):11-15,5.基金项目
国家自然科学基金资助项目(21502138) （21502138）
