作者:V. Venkatesh、Christopher J. Wedge、Isolda Romero-Canelón、Abraha Habtemariam、Peter J. Sadler
DOI:10.1039/c6dt01382a
日期:——
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
我们报告了硝基氧自旋标记的可光活化 Pt( IV ) 前药trans , trans , trans -[Pt(N 3 ) 2 (OH)(OCOCH 2 CH 2 CONH-TEMPO)(Py) 2 ] (Pt -TEMPO,其中 TEMPO = 2,2,6,6-四甲基哌啶 1-氧基)。用蓝色可见光照射产生 Pt( II ) 和叠氮基以及硝酰基自由基。Pt-TEMPO 在黑暗中表现出低毒性,但在光活化时对人卵巢癌细胞的活性与临床光敏剂氯丙嗪一样,并且在所用条件下比抗癌药物顺铂更具活性。