Synthesis and antitumor activity of novel CDDO derivatives
10.11665/j.issn.1000-5048.20170507
- VernacularTitle:新型CDDO衍生物的合成及抗肿瘤活性
- Author:
Jianghong PEI
1
;
Yu XIAO
;
Qixing LI
;
Zihao ZHAO
;
Li CHEN
Author Information
1. 中国药科大学天然药物化学教研室
- Keywords:
CDDO;
derivative;
synthesis;
antiproliferative activity;
plasma stability
- From:
Journal of China Pharmaceutical University
2017;48(5):548-553
- CountryChina
- Language:Chinese
-
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.
