"Click" Chemistry-Mediated Phenylene-Cored Carborane Dendrimers

被引:40
作者
Dash, Barada Prasanna [1 ]
Satapathy, Rashmirekha [1 ]
Bode, Barrie P. [2 ]
Reidl, Cory T. [1 ]
Sawicki, James W. [1 ]
Mason, Allen J. [1 ]
Maguire, John A. [3 ]
Hosmane, Narayan S. [1 ]
机构
[1] No Illinois Univ, Dept Chem & Biochem, De Kalb, IL 60115 USA
[2] No Illinois Univ, Dept Biol Sci, De Kalb, IL 60115 USA
[3] So Methodist Univ, Dept Chem, Dallas, TX 75275 USA
基金
美国国家科学基金会;
关键词
MEDICINAL CHEMISTRY; BORON CLUSTERS; DENDRONS; DELIVERY;
D O I
10.1021/om201255b
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
Phenylene-cored small dendrimers containing three to nine peripheral o-carborane clusters were synthesized via Cu(I)-catalyzed Huisgen-type azide alkyne cycloaddition reactions. The resulting dendrimers have been characterized by IR and NMR spectroscopy and MALDI-TOF mass spectral analysis. The biological evaluation of branched dendrimer 16 containing nine carborane cages has been carried out using human liver cancer cells (SK-Hep1). Dendrimer 16 was accumulated in the SK-Hep1 cancer cells in a concentration-dependent manner. The highest boron accumulation up to 2540 ng of boron/5 X 10(5) cells was observed at a 50 mu M concentration of 16 over a period of 20 h. The high accumulation of 16 into the tumor cell lines indicates that such dendritic boron drug delivery platforms could be possible for application in boron neutron capture therapy in cancer treatment.
引用
收藏
页码:2931 / 2935
页数:5
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