Reversing the undesirable pH-profile of doxorubicin via activation of a di-substituted maleamic acid prodrug at tumor acidity,Chemical Communications

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Reversing the undesirable pH-profile of doxorubicin via activation of a di-substituted maleamic acid prodrug at tumor acidity
Chemical Communications ( IF 4.3 ) Pub Date : 2017-11-01 00:00:00 , DOI: 10.1039/c7cc06843c
Anqi Zhang _{1,

2,

3,

4,

5} , Lan Yao _{3,

4,

6,

7,

8} , Ming An _{1,

2,

3,

4,

5}

Affiliation

The acid-labile behavior of di-substituted maleamic acid (DMA) and its equilibrium with di-substituted maleimide (DMI) are exploited to build an ultra acid-sensitive, small molecule prodrug that can be activated by tumor extracellular pH (pHe) in the range of 6.5–6.9. Such a DMA prodrug reversed the unfavorable pH-profile of doxorubicin (Dox), which may improve its therapeutic window.

中文翻译：

通过在肿瘤酸性下激活双取代的马来酰胺酸前药来逆转阿霉素的不良pH值

利用二取代马来酰胺酸（DMA）的酸不稳定行为及其与二取代马来酰亚胺（DMI）的平衡来建立一种对酸敏感的小分子前药，该前药可被肿瘤细胞外pH（pHe）激活。范围为6.5-6.9。这种DMA前药逆转了阿霉素（Dox）不利的pH谱，这可能会改善其治疗范围。

更新日期：2017-11-16

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