Heterocyclic N-oxidation Using Urea-Hydrogen Peroxide: a Safe, Convenient and Effective source of Hydrogen Peroxide.
D. Rong, V.A. Phillips, R.T. Wheelhouse. (2009) Current Issues in Organic Chemistry. Heron Press. 63-71.
Dr. Richard Wheelhouse
Reader
- Area
- School of Pharmacy & Medical Sciences
- Faculty of Life Sciences
- Phone
Biography
2016– Honorary Professor, Faculty of Pharmacy, University of Khartoum, Sudan.
2014– Reader in Medicinal Chemistry.
2006– EPSRC Peer Review College, nominated by the community.
Research
- Medicinal Chemistry
- Biophysics
- Anticancer Drugs
- Drug-Nucleic Acid Interactions
- Imidazotetrazines
- NMR
- UV
Research projects
Professional activities
- EPSRC Peer Review College, (1 January 2006)
- Brown Cancer Center, University of Louisville, Kentucky, USA - Visiting Research Scientist (1 April 2009)
- Bradford School of Pharmacy - Head, Division of Pharmaceutics and Pharmaceutical Chemistry (1 January 2006)
- Bradford School of Pharmacy - Lecturer (1 March 1998)
- The University of Texas at Austin, USA - Research Fellow (1 January 1996)
- The University of Nottingham, UK - Senior Research Fellow (1 January 1992)
- Aston University, Birmingham, UK - Research Associate (1 January 1990)
- Royal Society of Chemistry, CChem FRSC
- British Association for Cancer Research, member
Publications
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NMR and Molecular Modelling Studies on the Mechanism of Action of the Antitumour Drug Temozolomide.
R.T. Wheelhouse,* B.J. Denny, M.F.G. Stevens (1995) Contributions to Oncology 49: Novel Approaches in Anticancer Drug Design. S. Karger. 40-49.
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Synthesis and growth-inhibitory activities of imidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxamides related to the anti-tumour drug temozolomide, with appended silicon, benzyl and heteromethyl groups at the 3-position
David Cousin;Marc G. Hummersone;Tracey D. Bradshaw;Jihong Zhang;Christopher J. Moody;Magdalena B. Foreiter;Helen S. Summers;William Lewis;Richard T. Wheelhouse;Malcolm F. G. Stevens; (2018) MedChemComm.
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Evaluation of Novel Imidazotetrazine Analogues Designed to Overcome Temozolomide Resistance and Glioblastoma Regrowth
Ramirez, Y.P.; Mladek, A.C.; Phillips, Roger M.; Gynther, M.; Rautio, J.; Ross, A.H.; Wheelhouse, Richard T.; Sakaria, J.N. (2015) Molecular Cancer Therapeutics. 14
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Stabilization of a bimolecular triplex by 3'-S-phosphorothiolate modifications: An NMR and UV thermal melting investigation
Evans, K.;Bhamra, I.;Wheelhouse, R.T.;Arnold, J.R.P.;Cosstick, R.;Fisher, J.; (2015) CHEMISTRY - A EUROPEAN JOURNAL. 21
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The medicinal chemistry of imidazotetrazine prodrugs
Moody, C.L.;Wheelhouse, R.T.; (2014) Pharmaceuticals.
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Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA- methyltransferase, DNA mismatch repair, and p53
Pletsas, D.;Garelnabi, E.A.E.;Li, L.;Phillips, R.M.;Wheelhouse, R.T.; (2013) Journal of Medicinal Chemistry. 56
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Minor structural modifications to alchemix influence mechanism of action and pharmacological activity
Abdallah Q.;Phillips R.;Johansson F.;Helleday T.;Cosentino L.;Abdel-Rahman H.;Etzad J.;Wheelhouse R.;Kiakos K.;Bingham J.;Hartley J.;Patterson L.;Pors K. (2012) Biochemical Pharmacology. 83, 1514-1522.
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Probing the molecular recognition of a DNA·RNA hybrid duplex
Wheelhouse R.;Garbett N.;Buurma N.;Chaires J. (2010) Angewandte Chemie - International Edition. 49, 3207-3210.
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Polar, Functionalized Guanine-O6 Derivatives Resistant to Repair by O6-Alkylguanine-DNA Alkyltransferase: Implications for the Design of DNA-modifying Drugs.
Wheelhouse, Richard T.; Bibby, Michael C.; Nicolaou, Anna; Pletsas, Dimitrios (2009) European Journal of Medicinal Chemistry. 41
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A cytotoxic diterpenoid from Croton membranaceus, the major constituent of anticancer herbal formulations used in Ghana
Bayor, M.T.;Ayim, J.S.K.;Marston, G.;Phillips, R.M.;Shnyder, S.D.;Wheelhouse, R.T.;Wright, C.W.; (2008) Natural product communications.
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A safe, convenient and efficient method for the preparation of heterocyclic N-oxides using urea·hydrogen peroxide
Rong D.;Phillips V.;Rubio R.;Ángeles Castro M.;Wheelhouse R. (2008) Tetrahedron Letters. 49, 6933-6935.
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Inhibition of cobalamin-dependent methionine synthase by substituted benzo-fused heterocycles
Banks E.;Doughty S.;Toms S.;Wheelhouse R.;Nicolaou A. (2007) FEBS Journal. 274, 287-299.
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Design, synthesis, and evaluation of novel biarylpyrimidines: A new class of ligand for unusual nucleic acid structures
Wheelhouse R.;Jennings S.;Phillips V.;Pletsas D.;Murphy P.;Garbett N.;Chaires J.;Jenkins T. (2006) Journal of Medicinal Chemistry. 49, 5187-5198.
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In-vitro cytotoxic activities of the major bromophenols of the red alga Polysiphonia lanosa and some novel synthetic isomers
Shoeib N.;Bibby M.;Blunden G.;Linley P.;Swaine D.;Wheelhouse R.;Wright C. (2004) Journal of Natural Products. 67, 1445-1449.
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Biarylpyrimidines: a new class of ligand for high-order DNA recognition.
Murphy PM;Phillips VA;Jennings SA;Garbett NC;Chaires JB;Jenkins TC;Wheelhouse RT; (2003) CHEMICAL COMMUNICATIONS (PRINT).
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A novel, high-yielding synthesis of meso-substituted porphyrins via the direct arylation of porphine
Shi D.;Wheelhouse R. (2002) Tetrahedron Letters. 43, 9341-9342.
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A 15N NMR investigation of a series of benzotriazinones and related antitumour heterocycles
Vaughan, K.;Wilman, D.E.V.;Wheelhouse, R.T.;Stevens, M.F.G.; (2002) Magnetic Resonance in Chemistry.
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Quadruplex-interactive agents as telomerase inhibitors: Synthesis of porphyrins and structure-activity relationship for the inhibition of telomerase
Shi D.;Wheelhouse R.;Sun D.;Hurley L. (2001) Journal of Medicinal Chemistry. 44, 4509-4523.
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Antitumour imidazotetrazines. Part 39. Synthesis of bis(imidazotetrazine)s with saturated spacer groups
Arrowsmith J.;Jennings S.;Langnel D.;Wheelhouse R.;Stevens M. (2000) Journal of the Chemical Society, Perkin Transactions 1., 4432-4438.
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Effects of cationic porphyrins as G-quadruplex interactive agents in human tumor cells
Izbicka E.;Wheelhouse R.;Raymond E.;Davidson K.;Lawrence R.;Sun D.;Windle B.;Hurley L.;Von Hoff D. (1999) Cancer Research. 59, 639-644.
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Telomere-interactive agents affect proliferation rates and induce chromosomal destabilization in sea urchin embryos
Izbicka E.;Nishioka D.;Marcell V.;Raymond E.;Davidson K.;Lawrence R.;Wheelhouse R.;Hurley L.;Wu R.;Von Hoff D. (1999) Anti-Cancer Drug Design. 14, 355-365.
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Interactions of TMPyP4 and TMPyP2 with quadruplex DNA. Structural basis for the differential effects on telomerase inhibition
Han, F.X.;Wheelhouse, R.T.;Hurley, L.H.; (1999) Journal of the American Chemical Society.
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Cationic porphyrins as telomerase inhibitors: The interaction of tetra- (N-methyl-4-pyridyl)porphine with quadruplex DNA [1]
Wheelhouse, R.T.;Sun, D.;Han, H.;Han, F.X.;Hurley, L.H.; (1998) Journal of the American Chemical Society.
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Mechanism for the catalytic activation of ecteinascidin 743 and its subsequent alkylation of guanine N2
Moore II, B.M.;Seaman, F.C.;Wheelhouse, R.T.;Hurley, L.H.; (1998) Journal of the American Chemical Society.
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Antitumour imidazotetrazines. Part 36. Conversion of 5-aminoimidazole-4-carboxamide to imidazo[5,1-d][1,2,3,5]tetrazin-4(3H)-ones and imidazo[1,5-a][1,3,5]triazin-4(3H)-ones related in structure to the antitumour agents temozolomide and mitozolomide
Wang, Y.;Wheelhouse, R.T.;Zhao, L.;Langnel, D.A.F.;Stevens, M.F.G.; (1998) Journal of the Chemical Society, Perkin Transactions 1.
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Temozolomide: A review of its discovery, chemical properties, pre-clinical development and clinical trials
Newlands, E.S.;Stevens, M.F.G.;Wedge, S.R.;Wheelhouse, R.T.;Brock, C.; (1997) Cancer Treatment Reviews.
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Antitumour benzothiazoles. Part 4. An NMR study of the sites of protonation of 2-(4-aminophenyl)benzothiazoles
Wheelhouse, R.T.;Shi, D.-F.;Wilman, D.E.V.;Stevens, M.F.G.; (1996) Journal of the Chemical Society, Perkin Transactions 2.
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Structural studies on bioactive compounds. Part 27. Chemistry of the immunomodulatory agent bropirimine.
Stevens MF;Baig GU;Gate EN;Wheelhouse RT; (1995) Anti-Cancer Drug Design. 10
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Antitumour imidazotetrazines. Part 31. The synthesis of isotopically labelled temozolomide and a multinuclear (1H, 13C, 15N) magnetic resonance investigation of temozolomide and mitozolomide
R.T. Wheelhouse,* D.E.V. Wilman, W. Thomson, M.F.G. Stevens (1995) Journal of the Chemical Society, Perkin Transactions 1.
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Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide.
Clark AS;Deans B;Stevens MF;Tisdale MJ;Wheelhouse RT;Denny BJ;Hartley JA; (1995) Medicinal Chemistry.
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NMR and molecular modeling investigation of the mechanism of activation of the antitumor drug temozolomide and its interaction with DNA.
Denny BJ;Wheelhouse RT;Stevens MF;Tsang LL;Slack JA; (1994) Journal of Biochemistry.
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Decomposition of the antitumour drug temozolomide in deuteriated phosphate buffer: Methyl group transfer is accompanied by deuterium exchange
Wheelhouse, R.T.;Stevens, M.F.G.; (1993) Journal of the Chemical Society - Series Chemical Communications.
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Targeting of cytotoxic agents by polyamines: Synthesis of a chlorambucil-spermidine conjugate
Cohen, G.M.;Cullis, P.M.;Hartley, J.A.;Mather, A.;Symons, M.C.R.;Wheelhouse, R.T.; (1992) Chemical Communications.
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Targeting of tumor cells and DNA by a chlorambucil-spermidine conjugate.
Holley JL;Mather A;Wheelhouse RT;Cullis PM;Hartley JA;Bingham JP;Cohen GM; (1992) Cancer Research.
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Motion of polyammonium ions on aqueous solutions of DNA
Besley, S.;Cullis, P.M.;Partridge, R.;Symons, M.C.R.;Wheelhouse, R.T.; (1990) Chemical Physics Letters.
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The medicinal chemistry of imidazotetrazine prodrugs
Moody C.;Wheelhouse R. (2014) Pharmaceuticals.
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Glioblastoma multiforme therapy and mechanisms of resistance
Ramirez Y.;Weatherbee J.;Wheelhouse R.;Ross A. (2013) Pharmaceuticals.