Microwave gallium-68 radiochemistry for kinetically stable bis(thiosemicarbazone) complexes: structural investigations and cellular uptake under hypoxia

被引：25

作者：

Alam, Israt S. ^{[1
]}

Arrowsmith, Rory L. ^{[2
]}

Cortezon-Tamarit, Fernando ^{[2
]}

Twyman, Frazer ^{[1
]}

Kociok-Koehn, Gabriele ^{[2
]}

Botchway, Stanley W. ^{[3
]}

Dilworth, Jonathan R. ^{[4
]}

Carroll, Laurence ^{[1
]}

Aboagye, Eric O. ^{[1
]}

Pascu, Sofia I. ^{[2
]}

机构：

[1] Univ London Imperial Coll Sci Technol & Med, Dept Med, London W12 0NN, England

[2] Univ Bath, Dept Chem, Claverton Down BA2 7AY, England

[3] Oxford Brookes Univ, Rutherford Appleton Lab, Fac Hlth & Life Sci, Sci & Technol Facil Council, Oxford OX3 0BP, England

[4] Inorgan Chem Lab, Oxford OX2 6TT, England

来源：

DALTON TRANSACTIONS | 2016年 / 45卷 / 01期

关键词：

POSITRON-EMISSION-TOMOGRAPHY; ASSESSING TUMOR HYPOXIA; IN-VITRO; CONFOCAL FLUORESCENCE; ASSISTED SYNTHESIS; CERVICAL-CANCER; COPPER; THIOSEMICARBAZONES; DERIVATIVES; CU-60-ATSM;

D O I：

10.1039/c5dt02537k

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

We report the microwave synthesis of several bis(thiosemicarbazones) and the rapid gallium-68 incorporation to give the corresponding metal complexes. These proved kinetically stable under 'cold' and 'hot' biological assays and were investigated using laser scanning confocal microscopy, flow cytometry and radioactive cell retention studies under normoxia and hypoxia. Ga-68 complex retention was found to be 34% higher in hypoxic cells than in normoxic cells over 30 min, further increasing to 53% at 120 min. Our data suggests that this class of gallium complexes show hypoxia selectivity suitable for imaging in living cells and in vivo tests by microPET in nude athymic mice showed that they are excreted within 1 h of their administration.

引用

页码：144 / 155

页数：12