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A novel multifunctional 2-nitroimidazole-based bioreductive linker and its application in hypoxia-activated prodrugs.

Abstract：

:Tumor hypoxia has been widely explored over the years as a diagnostic and therapeutic marker. Herein, we designed, optimized and synthesized a new multifunctional bioreductive linker (12) containing an alkynyl group (potential click chemistry fragment); the linker is based on 2-nitroimidazole which was expected to simultaneously overcome the drawbacks of hypoxia-activated prodrugs (poor selectivity and unsatisfactory water solubility). Furthermore, a hypoxia-activated, water-soluble SN-38 prodrug was obtained, and it was stable under physiological conditions and was rapidly released as an active drug under hypoxic conditions.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Huang Y,Jin C,Yu J,Wang L,Lu W

doi

10.1016/j.bioorg.2020.103975

subject

Has Abstract

pub_date

2020-08-01 00:00:00

pages

103975

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)32211-4

journal_volume

101

pub_type

杂志文章

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