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Anticancer boron-containing prodrugs responsive to oxidative stress from the tumor microenvironment.

Abstract：

:Boronic acid (and ester) prodrugs targeting the overexpressed level of reactive oxygen species within tumor microenvironment represent a promising area for the discovery of new selective anticancer chemotherapy. This strategy that emerged only ten years ago is exponentially growing and could demonstrate its clinical usefulness in the near future. Herein, the previously described small-molecule and macromolecular anticancer prodrugs activated by carbon-boron oxidation are gathered. This review reports on the most interesting derivatives mentioned in the literature based on the in vitro and in vivo activity when available. Eventually, the pharmacological applicability of this strategy is discussed, in particular, the kinetic aspect of the prodrug oxidation and the selectivity of this reaction towards certain ROS from the tumor microenvironment are specified.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Maslah H,Skarbek C,Pethe S,Labruère R

doi

10.1016/j.ejmech.2020.112670

subject

Has Abstract

pub_date

2020-12-01 00:00:00

pages

112670

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(20)30642-5

journal_volume

207

pub_type

杂志文章,评审

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