Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10593573 | Bioorganic & Medicinal Chemistry Letters | 2013 | 4 Pages |
Abstract
The Ugi four-component reaction was used to prepare a series of artemisinin monomers and dimers. We found that the endoperoxide group in artemisinin remains intact during the reaction. The new artemisinin dimers showed potent anti-cancer activity against two human breast cancer cell lines, MDA-MB-231 and BT-474. One of the Ugi artemisinin dimers showed an IC50 value of 12Â nM when tested on BT474 cells, more than 600 times more potent than artesunate. Furthermore, the same Ugi artemisinin dimer showed a low toxicity when tested on MCF10A, a nontumorigenic cell line, resulting in a selectivity index of more than 8000.
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Shusheng Wang, Tomikazu Sasaki,