Spin-labelled photo-cytotoxic diazido platinum(IV) anticancer complex

V. Venkatesh; Christopher J. Wedge; Isolda Romero-Canelón; Abraha Habtemariam; Peter J. Sadler

doi:10.1039/c6dt01382a

Spin-labelled photo-cytotoxic diazido platinum(IV) anticancer complex

V. Venkatesh, Christopher J. Wedge, Isolda Romero-Canelón, Abraha Habtemariam, Peter J. Sadler

Research output: Contribution to journal › Article › peer-review

24 Citations (Scopus)

Abstract

We report the synthesis and characterisation of the nitroxide spin-labelled photoactivatable Pt(iv) prodrug trans,trans,trans-[Pt(N₃)₂(OH)(OCOCH₂CH₂CONH-TEMPO)(Py)₂] (Pt-TEMPO, where TEMPO = 2,2,6,6-tetramethylpiperidine 1-oxyl). Irradiation with blue visible light gave rise to Pt(ii) and azidyl as well as nitroxyl radicals. Pt-TEMPO exhibited low toxicity in the dark, but on photoactivation was as active towards human ovarian cancer cells as the clinical photosensitizer chlorpromazine and much more active than the anticancer drug cisplatin under the conditions used.

Original language	English
Pages (from-to)	13034-13037
Number of pages	4
Journal	Dalton Transactions
Volume	45
Issue number	33
Early online date	18 May 2016
DOIs	https://doi.org/10.1039/c6dt01382a
Publication status	Published - 2016
Externally published	Yes

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title = "Spin-labelled photo-cytotoxic diazido platinum(IV) anticancer complex",

abstract = "We report the synthesis and characterisation of the nitroxide spin-labelled photoactivatable Pt(iv) prodrug trans,trans,trans-[Pt(N3)2(OH)(OCOCH2CH2CONH-TEMPO)(Py)2] (Pt-TEMPO, where TEMPO = 2,2,6,6-tetramethylpiperidine 1-oxyl). Irradiation with blue visible light gave rise to Pt(ii) and azidyl as well as nitroxyl radicals. Pt-TEMPO exhibited low toxicity in the dark, but on photoactivation was as active towards human ovarian cancer cells as the clinical photosensitizer chlorpromazine and much more active than the anticancer drug cisplatin under the conditions used.",

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doi = "10.1039/c6dt01382a",

language = "English",

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T1 - Spin-labelled photo-cytotoxic diazido platinum(IV) anticancer complex

AU - Venkatesh, V.

AU - Wedge, Christopher J.

AU - Romero-Canelón, Isolda

AU - Habtemariam, Abraha

AU - Sadler, Peter J.

PY - 2016

Y1 - 2016

N2 - We report the synthesis and characterisation of the nitroxide spin-labelled photoactivatable Pt(iv) prodrug trans,trans,trans-[Pt(N3)2(OH)(OCOCH2CH2CONH-TEMPO)(Py)2] (Pt-TEMPO, where TEMPO = 2,2,6,6-tetramethylpiperidine 1-oxyl). Irradiation with blue visible light gave rise to Pt(ii) and azidyl as well as nitroxyl radicals. Pt-TEMPO exhibited low toxicity in the dark, but on photoactivation was as active towards human ovarian cancer cells as the clinical photosensitizer chlorpromazine and much more active than the anticancer drug cisplatin under the conditions used.

AB - We report the synthesis and characterisation of the nitroxide spin-labelled photoactivatable Pt(iv) prodrug trans,trans,trans-[Pt(N3)2(OH)(OCOCH2CH2CONH-TEMPO)(Py)2] (Pt-TEMPO, where TEMPO = 2,2,6,6-tetramethylpiperidine 1-oxyl). Irradiation with blue visible light gave rise to Pt(ii) and azidyl as well as nitroxyl radicals. Pt-TEMPO exhibited low toxicity in the dark, but on photoactivation was as active towards human ovarian cancer cells as the clinical photosensitizer chlorpromazine and much more active than the anticancer drug cisplatin under the conditions used.

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DO - 10.1039/c6dt01382a

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SP - 13034

EP - 13037

JO - Dalton Transactions

JF - Dalton Transactions

SN - 1477-9226

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ER -

Spin-labelled photo-cytotoxic diazido platinum(IV) anticancer complex

Abstract

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