期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 102, 期 -, 页码 180-187出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.07.040
关键词
Anti-cancer; Endoperoxide; Iron chelator; Conjugates
资金
- Jiangsu province 333 project
- Priority Academic Program Development of Jiangsu Higher Education Institutions
- Scientific Research Foundation for the Returned Overseas Chinese Scholars
- State Education Ministry
The effort to pursue effective anti-cancer drugs with novel mechanism of action has been continued for decades. As an antimalarial agent, artemisinin is well-known for its endoperoxide moiety, which is activated by the cellular iron. Meanwhile, the anti-cancer activity of artemisinin is recognized and reported. Herein, we report on the design, synthesis and evaluation of a series of endoperoxide and iron chelating moiety conjugates. Our study demonstrated that the endoperoxide-quinoline conjugates displayed effective antiproliferative capability and good selectivity against certain cancer cells, while both hydroxamate and catechol-endoperoxide conjugates shown no significant inhibitory activity. Preliminary mechanism investigation suggested that the antiproliferative activity of these conjugates is related to the endoperoxide moiety as well as their iron-chelating ability. These compounds are expected to be used as prototype for further development of selective anti-cancer drug candidate. (C) 2015 Elsevier Masson SAS. All rights reserved.
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