Expanding the Chemical Space of Withaferin A by Incorporating Silicon To Improve Its Clinical Potential on Human Ovarian Carcinoma Cells.

@article{Perestelo2019ExpandingTC,
  title={Expanding the Chemical Space of Withaferin A by Incorporating Silicon To Improve Its Clinical Potential on Human Ovarian Carcinoma Cells.},
  author={Nayra R. Perestelo and G. G. Llanos and C. P. Reyes and {\'A}ngel Amesty and K. Sooda and S. Afshinjavid and I. A. Jim{\'e}nez and F. Javid and I. L. Bazzocchi},
  journal={Journal of medicinal chemistry},
  year={2019},
  volume={62 9},
  pages={
          4571-4585
        }
}
Ovarian cancer represents the seventh most commonly diagnosed cancer worldwide. Herein, we report on the development of a withaferin A (WA)-silyl ether library with 30 analogues reported for the first time. Cytotoxicity assays on human epithelial ovarian carcinoma cisplatin-sensitive and -resistant cell lines identified eight analogues displaying nanomolar potency (IC50 ranging from 1 to 32 nM), higher than that of the lead compound and reference drug. This cytotoxic potency is also coupled… Expand