期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 25, 期 15, 页码 3057-3061出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2015.04.038
关键词
Necroptosis inducer; Tumor; E6; Biphenyl; SAR
资金
- National Natural Science Foundation of China [21072212]
- National Institute of Health of US [R37 AG012859]
Necroptosis inducers represent a promising potential treatment for drug-resistant cancer. We herein describe the structure modification of E6, which was identified recently as a potent and selective necroptosis inducer. The studies described herein demonstrate for the first time that functionalized biphenyl derivatives possess necroptosis inducer activity. Furthermore, these studies have led to the identification of two promising compounds (5h and 5j) that can be used for further optimization studies as well as mechanism of action investigations. (C) 2015 Elsevier Ltd. All rights reserved.
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