Tailored near-infrared contrast agents for image guided surgery.

Tailored near-infrared contrast agents for image guided surgery.
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DOI:
10.1021/acs.jmedchem.5b00253
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发表时间:
2015-03-26
影响因子:
7.3
通讯作者:
Henary, Maged
Henary, Maged
中科院分区:
医学1区
文献类型:
--
作者:
Njiojob, Costyl N.;Owens, Eric A.;Narayana, Lakshminarayana;Hyun, Hoon;Choi, Hak Soo;Henary, Maged

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The success of near-infrared (NIR) fluorescence to be employed for intraoperative imaging relies on the ability to develop a highly stable, NIR fluorescent, nontoxic, biocompatible, and highly excreted compound that retains a reactive functionality for conjugation to a cancer-recognizing peptide. Herein, systematic modifications to previously detailed fluorophore ZW800-1 are explored. Specific modifications, including the isosteric replacement of the O atom of ZW800-1, include nucleophilic amine and sulfur species attached to the heptamethine core. These novel compounds have shown similar satisfactory results in biodistribution and clearance while also expressing increased stability in serum. Most importantly, all of the synthesized and evaluated compounds display a reactive functionality (either a free amino group or carboxylic acid moiety) for further bioconjugation. The results obtained from the newly prepared derivatives demonstrate that the central substitution with the studied linking agents retains the ultralow background in vivo performance of the fluorophores regardless of the total net charge.
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