Dr Richard Wheelhouse
Reader
| Faculty/Dept/School |
School of Pharmacy and Medical Sciences (Faculty of Life Sciences) |
|---|---|
| r.t.wheelhouse@bradford.ac.uk | |
| Telephone | +441274 234710 |
Biography
2017– Associate Head, Internationalisation, School of Pharmacy and Medical Sciences,
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
| Date | Role | Title / Description | Funder | Award |
|---|---|---|---|---|
| - | PI | Imidazotetrazine Prodrugs | ||
| - | PI | Targeting DNA·RNA Hybrid Duplexes |
Professional activities
- 01-APR-09: Brown Cancer Center, University of Louisville, Kentucky, USA - Visiting Research Scientist
- 01-JAN-06: Bradford School of Pharmacy - Head, Division of Pharmaceutics and Pharmaceutical Chemistry
- 01-MAR-98: Bradford School of Pharmacy - Lecturer
- 01-JAN-96: The University of Texas at Austin, USA - Research Fellow
- 01-JAN-92: The University of Nottingham, UK - Senior Research Fellow
- 01-JAN-90: Aston University, Birmingham, UK - Research Associate
- Royal Society of Chemistry, CChem FRSC
- British Association for Cancer Research, member
- Editorial Board Member (Chemistry) Scientific Reports, Nature Publishing ,
- 01-JAN-06: EPSRC Peer Review College,
- 01-OCT-09: WO2009127815 - Aminoalkyl Imidazotetrazines for Treatment of Cancer
- 01-JAN-98: WO 98/33503 - Porphyrin Compounds as Telomerase Inhibitors
Publications
| Title | 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 (2018) |
|---|---|
| Authors | 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; |
| Journal | MedChemComm |
| DOI | 10.1039/c7md00554g |
| Title | Evaluation of Novel Imidazotetrazine Analogues Designed to Overcome Temozolomide Resistance and Glioblastoma Regrowth (2015) |
| Authors | Ramirez, Y.P.; Mladek, A.C.; Phillips, Roger M.; Gynther, M.; Rautio, J.; Ross, A.H.; Wheelhouse, Richard T.; Sakaria, J.N. |
| Journal | Molecular Cancer Therapeutics |
| Title | Stabilization of a bimolecular triplex by 3'-S-phosphorothiolate modifications: An NMR and UV thermal melting investigation (2015) |
| Authors | Evans, K.;Bhamra, I.;Wheelhouse, R.T.;Arnold, J.R.P.;Cosstick, R.;Fisher, J.; |
| Journal | CHEMISTRY - A EUROPEAN JOURNAL |
| DOI | 10.1002/chem.201500369 |
| Title | The medicinal chemistry of imidazotetrazine prodrugs (2014) |
| Authors | Moody, C.L.;Wheelhouse, R.T.; |
| Journal | Pharmaceuticals |
| DOI | 10.3390/ph7070797 |
| Title | Glioblastoma multiforme therapy and mechanisms of resistance (2013) |
| Authors | Ramirez Y.;Weatherbee J.;Wheelhouse R.;Ross A. |
| Journal | Pharmaceuticals |
| DOI | 10.3390/ph6121475 |
| Title | Synthesis and quantitative structure-activity relationship of imidazotetrazine prodrugs with activity independent of O6-methylguanine-DNA- methyltransferase, DNA mismatch repair, and p53 (2013) |
| Authors | Pletsas, D.;Garelnabi, E.A.E.;Li, L.;Phillips, R.M.;Wheelhouse, R.T.; |
| Journal | Journal of Medicinal Chemistry |
| DOI | 10.1021/jm401121k |
| Title | Minor structural modifications to alchemix influence mechanism of action and pharmacological activity (2012) |
| Authors | 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. |
| Journal | Biochemical Pharmacology |
| DOI | 10.1016/j.bcp.2012.02.017 |
| Title | Probing the molecular recognition of a DNA·RNA hybrid duplex (2010) |
| Authors | Wheelhouse R.;Garbett N.;Buurma N.;Chaires J. |
| Journal | Angewandte Chemie - International Edition |
| DOI | 10.1002/anie.200907235 |
| Title | Polar, Functionalized Guanine-O6 Derivatives Resistant to Repair by O6-Alkylguanine-DNA Alkyltransferase: Implications for the Design of DNA-modifying Drugs. (2009) |
| Authors | Wheelhouse, Richard T.; Bibby, Michael C.; Nicolaou, Anna; Pletsas, Dimitrios |
| Journal | European Journal of Medicinal Chemistry |
| Title | A cytotoxic diterpenoid from Croton membranaceus, the major constituent of anticancer herbal formulations used in Ghana (2008) |
| Authors | Bayor, M.T.;Ayim, J.S.K.;Marston, G.;Phillips, R.M.;Shnyder, S.D.;Wheelhouse, R.T.;Wright, C.W.; |
| Journal | Natural product communications |
| Title | A safe, convenient and efficient method for the preparation of heterocyclic N-oxides using urea·hydrogen peroxide (2008) |
| Authors | Rong D.;Phillips V.;Rubio R.;Ángeles Castro M.;Wheelhouse R. |
| Journal | Tetrahedron Letters |
| DOI | 10.1016/j.tetlet.2008.09.124 |
| Title | Inhibition of cobalamin-dependent methionine synthase by substituted benzo-fused heterocycles (2007) |
| Authors | Banks E.;Doughty S.;Toms S.;Wheelhouse R.;Nicolaou A. |
| Journal | FEBS Journal |
| DOI | 10.1111/j.1742-4658.2006.05583.x |
| Title | Design, synthesis, and evaluation of novel biarylpyrimidines: A new class of ligand for unusual nucleic acid structures (2006) |
| Authors | Wheelhouse R.;Jennings S.;Phillips V.;Pletsas D.;Murphy P.;Garbett N.;Chaires J.;Jenkins T. |
| Journal | Journal of Medicinal Chemistry |
| DOI | 10.1021/jm060315a |
| Title | In-vitro cytotoxic activities of the major bromophenols of the red alga Polysiphonia lanosa and some novel synthetic isomers (2004) |
| Authors | Shoeib N.;Bibby M.;Blunden G.;Linley P.;Swaine D.;Wheelhouse R.;Wright C. |
| Journal | Journal of Natural Products |
| DOI | 10.1021/np0305268 |
| Title | Biarylpyrimidines: a new class of ligand for high-order DNA recognition. (2003) |
| Authors | Murphy PM;Phillips VA;Jennings SA;Garbett NC;Chaires JB;Jenkins TC;Wheelhouse RT; |
| Journal | CHEMICAL COMMUNICATIONS (PRINT) |
| DOI | 10.1039/b301554h |
| Title | A novel, high-yielding synthesis of meso-substituted porphyrins via the direct arylation of porphine (2002) |
| Authors | Shi D.;Wheelhouse R. |
| Journal | Tetrahedron Letters |
| DOI | 10.1016/S0040-4039(02)02339-0 |
| Title | A 15N NMR investigation of a series of benzotriazinones and related antitumour heterocycles (2002) |
| Authors | Vaughan, K.;Wilman, D.E.V.;Wheelhouse, R.T.;Stevens, M.F.G.; |
| Journal | Magnetic Resonance in Chemistry |
| DOI | 10.1002/mrc.994 |
| Title | Quadruplex-interactive agents as telomerase inhibitors: Synthesis of porphyrins and structure-activity relationship for the inhibition of telomerase (2001) |
| Authors | Shi D.;Wheelhouse R.;Sun D.;Hurley L. |
| Journal | Journal of Medicinal Chemistry |
| DOI | 10.1021/jm010246u |
| Title | G-quadruplexes as targets for drug design (2000) |
| Authors | Hurley, L.H.;Wheelhouse, R.T.;Sun, D.;Kerwin, S.M.;Salazar, M.;Fedoroff, O.Y.;Han, F.X.;Han, H.;Izbicka, E.;Von Hoff, D.D.; |
| Journal | Pharmacology and Therapeutics |
| DOI | 10.1016/S0163-7258(99)00068-6 |
| Title | Antitumour imidazotetrazines. Part 39. Synthesis of bis(imidazotetrazine)s with saturated spacer groups (2000) |
| Authors | Arrowsmith J.;Jennings S.;Langnel D.;Wheelhouse R.;Stevens M. |
| Journal | Journal of the Chemical Society, Perkin Transactions 1 |
| DOI | 10.1039/b005652i |
| Title | Telomere-interactive agents affect proliferation rates and induce chromosomal destabilization in sea urchin embryos (1999) |
| Authors | Izbicka E.;Nishioka D.;Marcell V.;Raymond E.;Davidson K.;Lawrence R.;Wheelhouse R.;Hurley L.;Wu R.;Von Hoff D. |
| Journal | Anti-Cancer Drug Design |
| Title | Interactions of TMPyP4 and TMPyP2 with quadruplex DNA. Structural basis for the differential effects on telomerase inhibition (1999) |
| Authors | Han, F.X.;Wheelhouse, R.T.;Hurley, L.H.; |
| Journal | Journal of the American Chemical Society |
| DOI | 10.1021/ja984153m |
| Title | Effects of cationic porphyrins as G-quadruplex interactive agents in human tumor cells (1999) |
| Authors | Izbicka E.;Wheelhouse R.;Raymond E.;Davidson K.;Lawrence R.;Sun D.;Windle B.;Hurley L.;Von Hoff D. |
| Journal | Cancer Research |
| Title | Mechanism for the catalytic activation of ecteinascidin 743 and its subsequent alkylation of guanine N2 (1998) |
| Authors | Moore II, B.M.;Seaman, F.C.;Wheelhouse, R.T.;Hurley, L.H.; |
| Journal | Journal of the American Chemical Society |
| DOI | 10.1021/ja974109r |
| Title | 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 (1998) |
| Authors | Wang, Y.;Wheelhouse, R.T.;Zhao, L.;Langnel, D.A.F.;Stevens, M.F.G.; |
| Journal | Journal of the Chemical Society, Perkin Transactions 1 |
| Title | Cationic porphyrins as telomerase inhibitors: The interaction of tetra- (N-methyl-4-pyridyl)porphine with quadruplex DNA [1] (1998) |
| Authors | Wheelhouse, R.T.;Sun, D.;Han, H.;Han, F.X.;Hurley, L.H.; |
| Journal | Journal of the American Chemical Society |
| DOI | 10.1021/ja973792e |
| Title | Temozolomide: A review of its discovery, chemical properties, pre-clinical development and clinical trials (1997) |
| Authors | Newlands, E.S.;Stevens, M.F.G.;Wedge, S.R.;Wheelhouse, R.T.;Brock, C.; |
| Journal | Cancer Treatment Reviews |
| DOI | 10.1016/S0305-7372(97)90019-0 |
| Title | Antitumour benzothiazoles. Part 4. An NMR study of the sites of protonation of 2-(4-aminophenyl)benzothiazoles (1996) |
| Authors | Wheelhouse, R.T.;Shi, D.-F.;Wilman, D.E.V.;Stevens, M.F.G.; |
| Journal | Journal of the Chemical Society, Perkin Transactions 2 |
| Title | Structural studies on bioactive compounds. Part 27. Chemistry of the immunomodulatory agent bropirimine. (1995) |
| Authors | Stevens MF;Baig GU;Gate EN;Wheelhouse RT; |
| Journal | Anti-Cancer Drug Design |
| Title | Antitumor imidazotetrazines. 32. Synthesis of novel imidazotetrazinones and related bicyclic heterocycles to probe the mode of action of the antitumor drug temozolomide. (1995) |
| Authors | Clark AS;Deans B;Stevens MF;Tisdale MJ;Wheelhouse RT;Denny BJ;Hartley JA; |
| Journal | Medicinal Chemistry |
| DOI | 10.1021/jm00009a010 |
| Title | Antitumour imidazotetrazines. Part 31. The synthesis of isotopically labelled temozolomide and a multinuclear (1H, 13C, 15N) magnetic resonance investigation of temozolomide and mitozolomide (1995) |
| Authors | R.T. Wheelhouse,* D.E.V. Wilman, W. Thomson, M.F.G. Stevens |
| Journal | Journal of the Chemical Society, Perkin Transactions 1 |
| Title | NMR and molecular modeling investigation of the mechanism of activation of the antitumor drug temozolomide and its interaction with DNA. (1994) |
| Authors | Denny BJ;Wheelhouse RT;Stevens MF;Tsang LL;Slack JA; |
| Journal | Journal of Biochemistry |
| DOI | 10.1021/bi00197a003 |
| Title | Decomposition of the antitumour drug temozolomide in deuteriated phosphate buffer: Methyl group transfer is accompanied by deuterium exchange (1993) |
| Authors | Wheelhouse, R.T.;Stevens, M.F.G.; |
| Journal | Journal of the Chemical Society - Series Chemical Communications |
| Title | Targeting of tumor cells and DNA by a chlorambucil-spermidine conjugate. (1992) |
| Authors | Holley JL;Mather A;Wheelhouse RT;Cullis PM;Hartley JA;Bingham JP;Cohen GM; |
| Journal | Cancer Research |
| Title | Targeting of cytotoxic agents by polyamines: Synthesis of a chlorambucil-spermidine conjugate (1992) |
| Authors | Cohen, G.M.;Cullis, P.M.;Hartley, J.A.;Mather, A.;Symons, M.C.R.;Wheelhouse, R.T.; |
| Journal | Chemical Communications |
| Title | Motion of polyammonium ions on aqueous solutions of DNA (1990) |
| Authors | Besley, S.;Cullis, P.M.;Partridge, R.;Symons, M.C.R.;Wheelhouse, R.T.; |
| Journal | Chemical Physics Letters |
| DOI | 10.1016/0009-2614(90)85415-9 |
| Title | Heterocyclic N-oxidation Using Urea-Hydrogen Peroxide: a Safe, Convenient and Effective source of Hydrogen Peroxide. (2009) |
|---|---|
| Authors | D. Rong, V.A. Phillips, R.T. Wheelhouse. |
| Journal | Current Issues in Organic Chemistry |
| Publisher | Heron Press |
| Title | NMR and Molecular Modelling Studies on the Mechanism of Action of the Antitumour Drug Temozolomide. (1995) |
| Authors | R.T. Wheelhouse,* B.J. Denny, M.F.G. Stevens |
| Journal | Contributions to Oncology 49: Novel Approaches in Anticancer Drug Design |
| Publisher | S. Karger |
| Other type | Reviews |
|---|---|
| Title | The medicinal chemistry of imidazotetrazine prodrugs (2014) |
| Authors | Moody C.;Wheelhouse R. |
| Journal | Pharmaceuticals |
| DOI | 10.3390/ph7070797 |