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| 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 |
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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.
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Received: 05 January 2015
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2015, Vol. 23 
