中国药科大学学报2017，Vol.48Issue(5)：548-553,6.DOI:10.11665/j.issn.1000-5048.20170507
新型CDDO衍生物的合成及抗肿瘤活性
Synthesis and antitumor activity of novel CDDO derivatives
裴江鸿 1肖余 1李其星 1赵子豪 1陈莉1
作者信息
- 1. 中国药科大学天然药物化学教研室,南京210009
- 折叠
摘要
Abstract
Twelve novel 2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oic acid(CDDO) derivatives were designed and synthesized(9a-91) by introducing different heterocyclic rings to 17-COOH of CDDO through various linkers.Their structures were determined by ESI-MS,IR and 1 H NMR.The antiproliferative activity of the synthetic derivatives against human cancer cells HCT-116,A549 and HepG2 was evaluated by MTT assay.Several compounds showed potent inhibitory activities against test cell lines.Among them,compound 9c showed more potent antiproliferative activity than the CDDO-imidazolide (CDDO-Im).Moreover,rat plasma stability assay showed that compound 9c was more stable than CDDO-Im.关键词
2-氰基-3,12-二氧代齐墩果烷-1,9(11)-二烯-28-羧酸/衍生物/合成/抗增殖活性/血浆稳定性Key words
CDDO/derivative/synthesis/antiproliferative activity/plasma stability分类
医药卫生引用本文复制引用
裴江鸿,肖余,李其星,赵子豪,陈莉..新型CDDO衍生物的合成及抗肿瘤活性[J].中国药科大学学报,2017,48(5):548-553,6.
