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Roger C Whitehead

Explore the profile of Roger C Whitehead including associated specialties, affiliations and a list of published articles. Areas
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Articles 20
Citations 244
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Recent Articles
11.
Edwards A, Wagner C, Geist A, Burton N, Sharrad C, Adams R, et al.
Dalton Trans . 2016 Aug; 45(45):18102-18112. PMID: 27488559
The first examples of 4,7-disubstituted 2,9-bis(5,5,8,8-tetramethyl-5,6,7,8-tetrahydro-1,2,4-benzo-triazin-3-yl)-1,10-phenanthroline (CyMe-BTPhen) ligands are reported herein. Evaluating the kinetics, selectivity and stoichiometry of actinide(iii) and lanthanide(iii) radiotracer extractions has provided a mechanistic insight into the...
12.
Christou S, Ozturk E, Pritchard R, Quayle P, Stratford I, Whitehead R, et al.
Bioorg Med Chem Lett . 2013 Aug; 23(18):5066-9. PMID: 23937978
A synthetic approach to analogues of the terpenoid natural product antheminone A is described which employs (-)-quinic acid as starting material. A key conjugate addition step proved to be unpredictable...
13.
Lopez-Castejon G, Luheshi N, Compan V, High S, Whitehead R, Flitsch S, et al.
J Biol Chem . 2012 Dec; 288(4):2721-33. PMID: 23209292
IL-1β is a potent pro-inflammatory cytokine produced in response to infection or injury. It is synthesized as an inactive precursor that is activated by the protease caspase-1 within a cytosolic...
14.
McKibbin C, Mares A, Piacenti M, Williams H, Roboti P, Puumalainen M, et al.
Biochem J . 2011 Dec; 442(3):639-48. PMID: 22145777
Selective small-molecule inhibitors represent powerful tools for the dissection of complex biological processes. ES(I) (eeyarestatin I) is a novel modulator of ER (endoplasmic reticulum) function. In the present study, we...
15.
Dunstan M, Barnes J, Humphries M, Whitehead R, Bryce R, Leys D, et al.
J Med Chem . 2011 Aug; 54(19):6597-611. PMID: 21859103
Imidazoacridin-6-ones are shown to be potent nanomolar inhibitors of the enzyme NQO2. By use of computational molecular modeling, a reliable QSAR was established, relating inhibitory potency with calculated binding affinity....
16.
Nolan K, Humphries M, Barnes J, Doncaster J, Caraher M, Tirelli N, et al.
Bioorg Med Chem . 2009 Dec; 18(2):696-706. PMID: 20036559
A range of triazoloacridin-6-ones functionalized at C5 and C8 have been synthesized and evaluated for ability to inhibit NQO1 and NQO2. The compounds were computationally docked into the active site...
17.
Nolan K, Doncaster J, Dunstan M, Scott K, Frenkel A, Siegel D, et al.
J Med Chem . 2009 Nov; 52(22):7142-56. PMID: 19877692
The synthesis is reported here of two novel series of inhibitors of human NAD(P)H quinone oxidoreductase-1 (NQO1), an enzyme overexpressed in several types of tumor cell. The first series comprises...
18.
Arthurs C, Raftery J, Whitby H, Whitehead R, Wind N, Stratford I
Bioorg Med Chem Lett . 2007 Sep; 17(21):5974-7. PMID: 17870533
The synthesis of 6-epi-COTC, a diastereoisomer of Streptomyces metabolite 2-crotonyloxymethyl-(4R,5R,6R)-4,5,6-trihydroxycyclohex-2-enone (COTC), is described. The anti-cancer activities of the novel analogue, in racemic and enantiomerically pure forms, are presented.
19.
Arthurs C, Wind N, Whitehead R, Stratford I
Bioorg Med Chem Lett . 2006 Dec; 17(2):553-7. PMID: 17174551
The syntheses of three novel analogues of the naturally occurring cytotoxic agent COTC are described and the results of bioassays of the target compounds against two lung cancer cell lines...
20.
Doncaster J, Etchells L, Kershaw N, Nakamura R, Ryan H, Takeuchi R, et al.
Bioorg Med Chem Lett . 2006 Mar; 16(11):2877-81. PMID: 16563761
An array of novel analogues of the marine oxylipins, the manzamenones and plakoridines, have been prepared in divergent fashion using an approach modelled on a biogenetic theory. Many of the...