Synthesis of Gd(III)-C-palmitamidomethyl-C′-DOTAMA-C6-o-carborane: a new dual agent for innovative MRI/BNCT applications

被引:23
作者
Aime, Silvio [2 ]
Barge, Alessandro [3 ]
Crivello, Antonella [2 ]
Deagostino, Annamaria [1 ]
Gobetto, Roberto [2 ]
Nervi, Carlo [2 ]
Prandi, Cristina [1 ]
Toppino, Antonio [1 ,2 ]
Venturello, Paolo [1 ]
机构
[1] Univ Turin, Dipartimento Chim Gen & Chim Organ, I-10125 Turin, Italy
[2] Univ Turin, IFM, Dipartimento Chim, I-10125 Turin, Italy
[3] Univ Turin, Dipartimento Sci & Tecnol Farmaco, I-10125 Turin, Italy
关键词
D O I
10.1039/b808804g
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
C-(2-Benzyloxy)-ethyl-C'-N-tert-butoxycarbonyl-aminomethyl-o-carborane (8), a potentially useful intermediate for BNCT, has been synthesised. This intermediate can be readily functionalised with several biological vectors and MRI contrast agents. In this work intermediate 8 has been functionalised with a palmityl chain for lipophilic targeting and with Gd(III)-DOTAMA-C-6-NH2 as MRI detector. This combination yielded Gd(III)-C-palmitamidomethyl-C'-DOTAMA-C-6-o-carborane (14) as a dual MRI-BNCT agent.
引用
收藏
页码:4460 / 4466
页数:7
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