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Fine-Feature Modifications to Strained Ruthenium Complexes Radically Alter Their Hypoxic Anticancer Activity†
Photochemistry and Photobiology ( IF 2.6 ) Pub Date : 2021-02-09 , DOI: 10.1111/php.13395 Houston D Cole 1 , John A Roque 1, 2 , Liubov M Lifshits 1 , Rachel Hodges 2 , Patrick C Barrett 2 , Dmytro Havrylyuk 3 , David Heidary 3 , Elamparuthi Ramasamy 1 , Colin G Cameron 1 , Edith C Glazer 3 , Sherri A McFarland 1
Photochemistry and Photobiology ( IF 2.6 ) Pub Date : 2021-02-09 , DOI: 10.1111/php.13395 Houston D Cole 1 , John A Roque 1, 2 , Liubov M Lifshits 1 , Rachel Hodges 2 , Patrick C Barrett 2 , Dmytro Havrylyuk 3 , David Heidary 3 , Elamparuthi Ramasamy 1 , Colin G Cameron 1 , Edith C Glazer 3 , Sherri A McFarland 1
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In an earlier study of π-expansive ruthenium complexes for photodynamic and photochemo-therapies, it was shown that a pair of structural isomers differing only in the connection point of a naphthalene residue exhibited vastly different biological activity. These isomers are further explored in this paper through the activity of their functionalized derivatives. In normoxia, the inactive 2-NIP isomer (5) can be made as photocytotoxic as the active 1-NIP isomer (1) by functionalizing with methyl or methoxy groups, while methoxy variants of the 1-NIP isomer became inactive. In all cases, the singlet oxygen sensitization quantum yield was below 1%. Hypoxic photocytotoxicity was attenuated, with only three of the series showing any activity, notwithstanding the photodissociative ligands. The results here are consistent with the earlier findings in that seemingly minor structural modifications on the non-strained ligand can dramatically modulate the normoxic and hypoxic activity of these strained compounds and that these changes appear to exert a greater influence on photocytotoxicity than singlet oxygen sensitization or rates of photosubstitution in cell-free conditions would suggest.
中文翻译：
应变钌配合物的精细特征修饰从根本上改变了它们的低氧抗癌活性†
在一项用于光动力和光化学疗法的 π-膨胀型钌配合物的早期研究中，结果表明一对仅在萘残基连接点不同的结构异构体表现出截然不同的生物活性。本文通过其功能化衍生物的活性进一步探讨了这些异构体。在含氧量正常的情况下，非活性 2-NIP 异构体 ( 5 ) 可以像活性 1-NIP 异构体 ( 1 ) 一样具有光细胞毒性) 通过用甲基或甲氧基官能化，而 1-NIP 异构体的甲氧基变体变得不活跃。在所有情况下，单线态氧敏化量子产率均低于 1%。缺氧光细胞毒性减弱，尽管有光解离配体，但该系列中只有三个显示出任何活性。这里的结果与早期的发现一致，即在非应变配体上看似微小的结构修饰可以显着调节这些应变化合物的含氧量正常和低氧活性，并且这些变化似乎对光细胞毒性的影响比单线态氧敏化或无细胞条件下的光取代率会表明。
更新日期：2021-02-09
中文翻译：
应变钌配合物的精细特征修饰从根本上改变了它们的低氧抗癌活性†
在一项用于光动力和光化学疗法的 π-膨胀型钌配合物的早期研究中，结果表明一对仅在萘残基连接点不同的结构异构体表现出截然不同的生物活性。本文通过其功能化衍生物的活性进一步探讨了这些异构体。在含氧量正常的情况下，非活性 2-NIP 异构体 ( 5 ) 可以像活性 1-NIP 异构体 ( 1 ) 一样具有光细胞毒性) 通过用甲基或甲氧基官能化，而 1-NIP 异构体的甲氧基变体变得不活跃。在所有情况下，单线态氧敏化量子产率均低于 1%。缺氧光细胞毒性减弱，尽管有光解离配体，但该系列中只有三个显示出任何活性。这里的结果与早期的发现一致，即在非应变配体上看似微小的结构修饰可以显着调节这些应变化合物的含氧量正常和低氧活性，并且这些变化似乎对光细胞毒性的影响比单线态氧敏化或无细胞条件下的光取代率会表明。
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