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

Israt S. Alam; Rory L. Arrowsmith; Fernando Cortezon Tamarit; Frazer Twyman; Gabriele Kociok-köhn; Stanley W. Botchway; Jonathan R. Dilworth; Laurence Carroll; Eric O. Aboagye; Sofia I. Pascu

doi:10.1039/C5DT02537K

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

Israt S. Alam, Rory L. Arrowsmith, Fernando Cortezon Tamarit, Frazer Twyman, Gabriele Kociok-köhn, Stanley W. Botchway, Jonathan R. Dilworth, Laurence Carroll, Eric O. Aboagye, Sofia I. Pascu

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21 Citations (SciVal)

Abstract

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. 68Ga 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.

Original language	English
Pages (from-to)	144-155
Journal	Dalton Transactions
Volume	45
Issue number	1
DOIs	https://doi.org/10.1039/C5DT02537K
Publication status	Published - 7 Jan 2016

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10.1039/C5DT02537KLicence: CC BY

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Alam, I. S., Arrowsmith, R. L., Cortezon Tamarit, F., Twyman, F., Kociok-köhn, G., Botchway, S. W., Dilworth, J. R., Carroll, L., Aboagye, E. O., & Pascu, S. I. (2016). Microwave gallium-68 radiochemistry for kinetically stable bis(thiosemicarbazone) complexes: structural investigations and cellular uptake under hypoxia. Dalton Transactions , 45(1), 144-155. https://doi.org/10.1039/C5DT02537K

Alam, IS, Arrowsmith, RL, Cortezon Tamarit, F, Twyman, F, Kociok-köhn, G, Botchway, SW, Dilworth, JR, Carroll, L, Aboagye, EO & Pascu, SI 2016, 'Microwave gallium-68 radiochemistry for kinetically stable bis(thiosemicarbazone) complexes: structural investigations and cellular uptake under hypoxia', Dalton Transactions , vol. 45, no. 1, pp. 144-155. https://doi.org/10.1039/C5DT02537K

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abstract = "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 {\textquoteleft}cold{\textquoteright} and {\textquoteleft}hot{\textquoteright} biological assays and were investigated using laser scanning confocal microscopy, flow cytometry and radioactive cell retention studies under normoxia and hypoxia. 68Ga 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.",

author = "Alam, {Israt S.} and Arrowsmith, {Rory L.} and {Cortezon Tamarit}, Fernando and Frazer Twyman and Gabriele Kociok-k{\"o}hn and Botchway, {Stanley W.} and Dilworth, {Jonathan R.} and Laurence Carroll and Aboagye, {Eric O.} and Pascu, {Sofia I.}",

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AU - Alam, Israt S.

AU - Arrowsmith, Rory L.

AU - Cortezon Tamarit, Fernando

AU - Twyman, Frazer

AU - Kociok-köhn, Gabriele

AU - Botchway, Stanley W.

AU - Dilworth, Jonathan R.

AU - Carroll, Laurence

AU - Aboagye, Eric O.

AU - Pascu, Sofia I.

PY - 2016/1/7

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N2 - 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. 68Ga 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.

AB - 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. 68Ga 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.

UR - http://dx.doi.org/10.1039/C5DT02537K

UR - https://doi.org/10.1039/C5DT02537K

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DO - 10.1039/C5DT02537K

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JO - Dalton Transactions

JF - Dalton Transactions

IS - 1

ER -

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

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