Interrogation of the Structure–Activity Relationship of a Lipophilic Nitroaromatic Prodrug Series Designed for Cancer Gene Therapy Applications

Interrogation of the Structure–Activity Relationship of a Lipophilic Nitroaromatic Prodrug Series Designed for Cancer Gene Therapy Applications

PR-104A is a dual hypoxia/nitroreductase gene therapy prodrug by virtue of its ability to undergo either one- or two-electron reduction to its cytotoxic species. It has been evaluated extensively in pre-clinical GDEPT studies, yet off-target human aldo-keto reductase AKR1C3-mediated activation has l...

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Bibliographic Details
Main Authors: Amir Ashoorzadeh, Alexandra M. Mowday, Christopher P. Guise, Shevan Silva, Matthew R. Bull, Maria R. Abbattista, Janine N. Copp, Elsie M. Williams, David F. Ackerley, Adam V. Patterson, Jeff B. Smaill
Format: Article
Language:English
Published: MDPI AG 2022-02-01
Series:Pharmaceuticals
Subjects:
nitrobenzamide
mustard
prodrug
SAR
bystander effect
cancer gene therapy
Online Access:https://www.mdpi.com/1424-8247/15/2/185

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