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Synthesis and anti-tumor activity evaluation of ent-6,7-seco-oridonin derivatives
LI Dahong 1 #,WANG Lei 2,CAI Hao 3,WU Xiaoming 2,SUN Yijun 3,XU Jinyi 2 *
1.Department of Medicinal Chemistry, China Pharmaceutical University, NanJing 210009
2.State Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009
3.Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009
*Correspondence author
#Submitted by
Subject:
Funding: Project for Research and Innovation of Graduates in Universities of Jiangsu Province (No.CXZZ11-0800), National Natural Science Fund (No.No. 30973610), Specialized Research Fund for the Doctoral Program of Higher Education (No.No. 20100096110001), the Fundamental Research Funds for the Central Universities (No.JKY2011030)
Opened online:24 July 2012
Accepted by: none
Citation: LI Dahong,WANG Lei,CAI Hao.Synthesis and anti-tumor activity evaluation of ent-6,7-seco-oridonin derivatives[OL]. [24 July 2012] http://en.paper.edu.cn/en_releasepaper/content/4483740
 
 
This paper presents the synthesis of ent-6,7-seco-oridonin derivatives from commercial available natural product oridonin (1) and their biological activities were evaluated. The results demonstrated that the most effective compound 11 has improved =anti-proliferative activity than oridonin and similar potency compared with Taxol in A549 cell and Bel-7402 cell with IC50 of 4.58 and 5.03 μM, respectively. Compound 11 was also more potent than parent compound oridonin in mice with MGC-803 gastric cancer in vivo. These results would provide valuable information in the novel anticancer drugs development.
Keywords:ent-6,7-seco-oridonin; derivative; anti-tumor activity
 
 
 

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