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Bradford, United Kingdom

Elliott E.-C.,University of Liverpool | Elliott E.-C.,Unilever | Regan S.L.,University of Liverpool | Regan S.L.,Unilever | And 9 more authors.
Journal of Medicinal Chemistry | Year: 2012

The anticonvulsant carbamazepine 1 is associated with adverse drug reactions (ADRs), including hepatotoxicity; oxidative metabolism of 1 has been implicated in the pathogenesis of the ADRs. We report the synthesis and evaluation of 2-monohalo and 2,8-dihalo analogues of 1 that were intended to minimize reactive metabolite formation via arene oxidation and 10,11-epoxidation. Halo analogues were obtained either by rearrangement of halogenated N-arylindoles or from specifically halogenated iminodibenzyl derivatives. In rat hepatocytes, none of the analogues underwent oxidative dehalogenation or glutathione adduction. Some formation of the 10,11-epoxide still occurred, but aromatic hydroxylation was not seen with the exception of 2-fluoro, which allowed minor monohydroxylation. Complete inhibition of aromatic hydroxylation required at least monochlorination or difluorination of 1. In human liver microsomes, difluoro analogue 5b underwent 10,11-epoxidation but gave no arene oxidation. © 2012 American Chemical Society. Source


Donnelly O.G.,University of Leeds | Donnelly O.G.,Mayo Medical School | Errington-Mais F.,University of Leeds | Steele L.,University of Leeds | And 13 more authors.
Gene Therapy | Year: 2013

Oncolytic viruses (OV) are promising treatments for cancer, with several currently undergoing testing in randomised clinical trials. Measles virus (MV) has not yet been tested in models of human melanoma. This study demonstrates the efficacy of MV against human melanoma. It is increasingly recognised that an essential component of therapy with OV is the recruitment of host antitumour immune responses, both innate and adaptive. MV-mediated melanoma cell death is an inflammatory process, causing the release of inflammatory cytokines including type-1 interferons and the potent danger signal HMGB1. Here, using human in vitro models, we demonstrate that MV enhances innate antitumour activity, and that MV-mediated melanoma cell death is capable of stimulating a melanoma-specific adaptive immune response. © 2013 Macmillan Publishers Limited All rights reserved. Source


Vinader V.,Institute of Cancer Therapeutics | Afarinkia K.,Institute of Cancer Therapeutics
Future Medicinal Chemistry | Year: 2012

This review provides an overview of chemokines and their receptors, with an emphasis on general features and nomenclature along with a short summary of their properties and functions. It is intended as an introduction to the subject and a reference point for those wishing to learn key facts about chemokines and their role in biology. © 2012 Future Science Ltd. Source


Afarinkia K.,Institute of Cancer Therapeutics | Royappa M.,Institute of Cancer Therapeutics | Scowen I.J.,University of Bradford
Phosphorus, Sulfur and Silicon and the Related Elements | Year: 2011

A general method for the synthesis of novel oligomers comprising α-hydroxy and α-amino phenylphosphinic acid building blocks is reported. A series of dimeric α-hydroxy phenylphosphinates is analyzed by a combination of NMR, X-ray crystallography, and computational methods. Copyright © Taylor & Francis Group, LLC. Source


Afarinkia K.,Institute of Cancer Therapeutics | Royappa M.,Institute of Cancer Therapeutics | Scowen I.J.,University of Bradford | Steed J.W.,Durham University | Yu H.-W.,Institute of Cancer Therapeutics
Organic and Biomolecular Chemistry | Year: 2010

A general method for the synthesis of a novel class of oligomers, comprising α-hydroxy phenylphosphinic acid building blocks, is reported. A series of dimeric α-hydroxy phenylphosphinates are analyzed by a combination of NMR spectroscopy, X-ray crystallography and computational methods. © 2010 The Royal Society of Chemistry. Source

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