期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 93, 期 -, 页码 172-181出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.01.064
关键词
Phosphate inositol; Bioreversible protection; 4-Acyloxybenzyl; Anticancer
资金
- Tianjin Municipal Natural Science Foundation [12JCZDJC22000]
- Ministry of Science and Technology of China [2010CB126102, 2011BAE06B05]
- National Science Foundation for Fostering Talents in Basic Research of the National Natural Science Foundation of China (NFFTBS) [J1103306]
The chemistry and biology of phosphorylated inositols have become intense areas of research during the last two decades due to their involvement in various cellular signaling processes. However, the metabolic instability by phosphatases or kinases and poor penetration make it difficult to become a drug used in the clinic. The bioreversible protection technique can enhance membrane penetration characteristics and increase the stability of phosphorylated inositols against enzymatic degradation and is applied widely in drug discovery and development. In this paper, we described the design and synthesis of 22 bioreversible phosphotriester inositols, along with the initial antitumor activity results. Most compounds exhibited significant cytotoxic activity against human cancer cell lines A549, MDA-MB-231 and HeLa, but lower cellular toxicity on normal cell MCF10A in comparison with Cisplatin. These compounds can be used as probes to study the mechanism of intracellular signal transduction mediated by phosphate inositol or as leads of phosphate inositol drugs in the clinic. (C) 2015 Elsevier Masson SAS. All rights reserved.
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