期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 83, 期 -, 页码 389-397出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.06.005
关键词
Alkynes; Carboranes; Boron neutron capture therapy; Antitumor agents; Drug research
资金
- Ministry of Education, Youth and Sports of the Czech Republic [LC06070, 1M0508, P207/13/159155, MSM0021620857]
- National Science Foundation [CHE-0906179]
- Kishwaukee Community Hospital Foundation
The syntheses of the unprotected neutral closo-carboranyl-C-deoxyriboses, starting from anomeric mixture of 1-ethynyldeoxyriboses, and their corresponding open-cage nido-derivatives have been described. The structures of both the alpha- and beta-anomers were confirmed by single-crystal X-ray diffraction. While limited water solubility of the neutral closo-anomers led to high cytotoxicity, their cesium salts (nido-species) exhibited higher water solubility leading to lower cytotoxicity. However, in vitro boron neutron capture therapy (BNCT) investigation using the murine squamous cell carcinoma (SCCVII) cell lines showed that there are no significant differences between the survival fractions of the two species. (C) 2014 Elsevier Masson SAS. All rights reserved.
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