1. 广州医科大学 a. 药学院(广东 广州 511436)； b. 附属第三医院（广东 广州 510150）； c. 实验医学研究中心（广东 广州 511436）
Synthesis and Antitumor Activities of Novel Aryl-substituted Gambogic Acid Derivatives
ZHANG Zhi-jia1a,1b, LI Jin-hai1a, CHEN Mei-jun1a, HUANG Yan1a, ZHAO Lu-ning1c
a. School of Pharmaceutical Science（Guangzhou 511436）; b. The Third Affiliated Hospital（Guangzhou 510150）； c. Experimental Medical Research Center（Guangzhou 511436）， 1. Guangzhou Medical University, Guangzhou, China
Abstract：Aryloxy（heterocyclic）-alcohol（2a~2k） were prepared by Williamson ether reaction of substituted phenols(or hydroxypyridines) with bromo-alcohol, using K2CO3 as alkali. Gambogic acid derivatives(3a~3k) were synthesized by Mitsunobu reaction of 2a~2m with gambogic acid, respectively. Arycarbonylamibo alcohols（5a~5h) were prepared by coupling reaction of aromatic acid with 3-amino-1-propanol, using DDC/HOSu as coupling agent. Gambogic acid derivatives(6a~6h) were synthesized by Mitsunobu reaction of 5a~5h with gambogic acid, respectively. 2, 3, 5 and 6 were new compounds and the structures were characterized by 1H NMR, ESI-MS and HR-MS. The in vitro antitumor activities of 3 and 6 against human lung cancer cells(A549), human liver cancer cells(HepG-2) and human breast cancer cells(SK-BR-3) were investigated by MTT method. The results showed that some of the compounds exhibited better antitumor activities than gambogic acid.
2015, Vol. 23 
