Synthesis and screening of novel vitamin E derivatives for anticancer functions
- Eur J Med Chem. 2012 Dec:58:72-83. doi: 10.1016/j.ejmech.2012.09.045.
- 1. School of Biological Sciences/C0900, University of Texas at Austin, Austin 78712, TX, USA.
α-TEA, RRR-α-tocopherol ether linked acetic acid, exhibits potent Anticancer actions in vitro and in vivo; whereas, the parent molecule has no Anticancer activity. In this study, we incorporated fluorine at the chroman head and/or ether linkage between the chroman head and phytyl tail of α-TEA as well as RRR-α-tocopherol to synthesize 6 vitamin E derivatives, and evaluated the Anticancer actions in vitro for ability to induce cell death by Apoptosis of human MCF-7 and MDA-MB-231 Breast Cancer cell lines and mouse mammary Cancer cell line 66cl-4GFP. All derivatives, with the exception of compound 12, exhibited Anticancer properties. The modified α-TEA ether-type phytyl group exhibited the highest pro-apoptotic activity in comparison with α-TEA as well as other vitamin E derivatives.