Hypoxia-activated prodrugs: paths forward in the era of personalised medicine

FW Hunter, BG Wouters, WR Wilson - British journal of cancer, 2016 - nature.com
Tumour hypoxia has been pursued as a cancer drug target for over 30 years, most notably
using bioreductive (hypoxia-activated) prodrugs that target antineoplastic agents to low …

Enzyme-catalyzed activation of anticancer prodrugs

M Rooseboom, JNM Commandeur… - Pharmacological …, 2004 - Elsevier
The rationale for the development of prodrugs relies upon delivery of higher concentrations
of a drug to target cells compared to administration of the drug itself. In the last decades …

The chemical and biological activities of quinones: overview and implications in analytical detection

N El-Najjar, H Gali-Muhtasib, RA Ketola… - Phytochemistry …, 2011 - Springer
Quinones are a class of natural and synthetic compounds that have several beneficial
effects. Quinones are electron carriers playing a role in photosynthesis. As vitamins, they …

[HTML][HTML] Hypoxia-activated prodrugs and (lack of) clinical progress: The need for hypoxia-based biomarker patient selection in phase III clinical trials

L Spiegelberg, R Houben, R Niemans… - Clinical and translational …, 2019 - Elsevier
Hypoxia-activated prodrugs (HAPs) are designed to specifically target the hypoxic cells of
tumors, which are an important cause of treatment resistance to conventional therapies …

Prodrug strategies in cancer therapy

WA Denny - European journal of medicinal chemistry, 2001 - Elsevier
Systemic cytotoxic (anti-proliferative) anticancer drugs rely primarily for their therapeutic
effect on cytokinetic differences between cancer and normal cells. One approach aimed at …

Bioreductive prodrugs as cancer therapeutics: targeting tumor hypoxia

CP Guise, AM Mowday, A Ashoorzadeh… - Chinese journal of …, 2014 - pmc.ncbi.nlm.nih.gov
Hypoxia, a state of low oxygen, is a common feature of solid tumors and is associated with
disease progression as well as resistance to radiotherapy and certain chemotherapeutic …

Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302

F Meng, JW Evans, D Bhupathi, M Banica… - Molecular cancer …, 2012 - aacrjournals.org
Abstract TH-302 is a 2-nitroimidazole triggered hypoxia-activated prodrug (HAP) of bromo-
isophosphoramide mustard currently undergoing clinical evaluation. Here, we describe …

Quinoxaline 1,4-di-N-Oxides: Biological Activities and Mechanisms of Actions

G Cheng, W Sa, C Cao, L Guo, H Hao, Z Liu… - Frontiers in …, 2016 - frontiersin.org
Quinoxaline 1, 4-di-N-oxides (QdNOs) have manifold biological properties, including
antimicrobial, antitumoral, antitrypanosomal and antiinflammatory/antioxidant activities …

Taking advantage of tumor cell adaptations to hypoxia for develo** new tumor markers and treatment strategies

P Ebbesen, EO Pettersen, TA Gorr, G Jobst… - Journal of enzyme …, 2009 - Taylor & Francis
Cancer cells in hypoxic areas of solid tumors are to a large extent protected against the
action of radiation as well as many chemotherapeutic drugs. There are, however, two …

Bioreductive drugs: from concept to clinic

SR McKeown, RL Cowen, KJ Williams - Clinical oncology, 2007 - Elsevier
One of the key issues for radiobiologists is the importance of hypoxia to the radiotherapy
response. This review addresses the reasons for this and primarily focuses on one aspect …