Sunderland Repository records the research produced by the University of Sunderland including practice-based research and theses.
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Lloyd, Matthew D, Yevglevskis, Maksims, Nathubhai, Amit, James, Tony D, Threadgill, Michael D and Woodman, Timothy J (2021) Racemases and epimerases operating through a 1,1-proton transfer mechanism: reactivity, mechanism and inhibition. Chemical Society reviews, 50 (10). pp. 5952-5984. ISSN 1460-4744
Petrova, Yoana, D., Wadda, Katty, Nathubhai, Amit, Yevglevskis, Maksims, Mitchell, Paul, J., James, Tony, D., Threadgill, Michael, D., Woodman, Timothy, J. and Lloyd, Matthew, D. (2019) Identification of novel small-molecule inhibitors of α-methylacyl-CoA racemase (AMACR; P504S) and structure activity relationships. Bioorganic Chemistry, 92 (103264). pp. 1-6. ISSN 0045-2068
Yevglevskis, Maksims, Nathubhai, Amit, Wadda, Katty, Lee, Guat, Al-Rawi, Suzanne, Jiao, Tingying, Mitchell, Paul, J., James, Tony, D., Threadgill, Michael, D., Woodman, Timothy, J. and Lloyd, Matthew, D. (2019) Novel 2-arylthiopropanoyl-CoA inhibitors of α-methylacyl-CoA racemase 1A (AMACR; P504S) as potential anti-prostate cancer agents. Bioorganic Chemistry, 92 (103263). pp. 1-8. ISSN 0045-2068
Yevglevskis, M., Lee, G. L, Nathubhai, Amit, Petrova, Y.D., James, T.D., Threadgill, M.D., Woodman, T.J and Lloyd, M.D. (2018) Structure-activity relationships of rationally designed AMACR 1A inhibitors. BIOORGANIC CHEMISTRY, 79. pp. 145-154. ISSN 0045-2068
Gravells, P., Neale, J., Grant, E., Nathubhai, Amit, Smith, K.M., James, D.I. and Bryant, H.E. (2018) Radiosensitization with an inhibitor of poly(ADP-ribose) glycohydrolase: A comparison with the PARP1/2/3 inhibitor olaparib. DNA Repair, 61. pp. 25-36. ISSN 1568-7864
Yevglevskis, M., Lee, G.L., Nathubhai, Amit, Petrova, Y.D., James, T.D., Threadgill, M.D., Woodman, T.J. and Lloyd, M.D. (2017) A novel colorimetric assay for alpha-methylacyl-CoA racemase 1A (AMACR; P504S) utilizing the elimination of 2,4-dinitrophenolate. Chemical Communications, 53 (37). pp. 5073-5240. ISSN 1359-7345
Nathubhai, Amit, Haikarainen, T., Koivunen, J., Murthy, S., Koumanov, F., Lloyd, M.D., Holman, J.D., Pihlajaniemi, T., Tosh, D., Lehtiö, L. and Threadgill, M.D. (2017) Highly Potent and Isoform Selective Dual Site Binding Tankyrase/Wnt Signaling Inhibitors That Increase Cellular Glucose Uptake and Have Antiproliferative Activity. Journal of Medicinal Chemistry, 60 (2). pp. 814-820. ISSN 0022-2623
Nathubhai, Amit, Threadgill, M D (2016) New potent and selective tankyrase inhibitors for the treatment of disease or conditions associated with Wnt signalling e.g. colon cancer, prostate cancer, idiopathic pulmonary fibrosis, chronic obstructive pulmonary disease and type-1/type-2 diabetes. WO2017-GB52624.
Nathubhai, Amit, Haikarainen, T, Hayward, P.C., Munoz-Descalzo, S., Thompson, A.S., Lloyd, M.D., Lehtio, L. and Threadgill, M.D. (2016) Structure-activity relationships of 2-arylquinazolin-4-ones as highly selective and potent inhibitors of the tankyrases. European Journal of Medicinal Chemistry, 118. pp. 316-327. ISSN 0223-5234
Paine, H.A., Nathubhai, Amit, Woon, E.C.Y., Sunderland, P.T., Wood, P.J., Mahon, M.F., Lloyd, M.D., Thompson, A.S., Haikarainen, T., Narwal, M., Lehtiö, L. and Threadgill, M.D. (2015) Exploration of the nicotinamide-binding site of the tankyrases,identifying 3-arylisoquinolin-1-ones as potent and selective inhibitors in vitro. Bioorganic & Medicinal Chemistry, 23. pp. 5891-5908. ISSN 0968-0896
Kumpan, K., Nathubhai, Amit, Zhang, C., Wood, P.J., Lloyd, M.D., Thompson, A.S., Haikarainen, T., Lehtiö, L. and Threadgill, M.D. (2015) Structure-based design, synthesis and evaluation in vitro of arylnaphthyridinones, arylpyridopyrimidinones and their tetrahydro derivatives as inhibitors of the tankyrases. Bioorganic & Medicinal Chemistry, 23. pp. 3013-3032. ISSN 0968-0896
Twum, E.A., Nathubhai, Amit, Wood, P.J., Lloyd, M.D., Thompson, A.S. and Threadgill, M.D. (2015) Initial development of a cytotoxic amino-seco-CBI warhead for delivery by prodrug systems. Bioorganic & Medicinal Chemistry, 23. pp. 3481-3489. ISSN 0968-0896
Nathubhai, Amit, Wood, P.J., Lloyd, M.D., Thompson, A.S. and Threadgill, M.D. (2013) Design and Discovery of 2‑Arylquinazolin-4-ones as Potent and Selective Inhibitors of Tankyrases. ACS Medicinal Chemistry Letters, 4 (12). pp. 1173-1177. ISSN 1948-5875
Threadgill, M D, Lloyd, M D, Thompson, A S, Nathubahai, Amit, Wood, P J, Paine, H A, Kumpan, E, Sunderland. P T, Woon, Y, Chue, E (2013) Use of new and known pyridine or pyrimidine compounds, for the treatment of a disease or condition associated with tankyrase, e.g. cancer selected from e.g. breast, colon, stomach, and liver. WO2014087165A1.
Nathubhai, Amit, Patterson, R., Woodman, T.J., Sharp, H.E.C., Chui, M.T.Y., Chung, H.H.K., Lau, W.S., Zheng, J., Lloyd, M.D., Thompson, A.S. and Threadgill, M.D. (2011) N3-Alkylation during formation of quinazolin-4-ones from condensation of anthranilamides and orthoamides. Organic & Biomolecular Chemistry, 9. pp. 6089-6099. ISSN 1477-0520
Dixon, M.J., Nathubhai, Amit, Andersen, O.A., van Aalten, D.M.F. and Eggleston, I.M. (2009) Synthesis and structure-based dissection of cyclic peptide chitinase inhibitors: New leads for antifungal and anti-inflammatory drugs. Advances in Experimental Medicine and Biology, 611. pp. 525-526. ISSN 0065-2598
Dixon, M.J., Nathubhai, Amit, Andersen, O.A., van Aalten, D.M.F. and Eggleston, I.M. (2008) Solid-phase synthesis of cyclic peptide chitinase inhibitors: SAR of the argifin scaffold. Organic & Biomolecular Chemistry, 7. pp. 259-268. ISSN 1477-0520
Dixon, M.J., Giuntini, F., Nathubhai, Amit, Andersen, O.A., van Aalten, D.M.F. and Eggleston, I.M. (2008) Synthetic approaches to cyclic peptide natural products as chitinase inhibitors. Journal of Peptide Science, 14 (8). p. 55. ISSN 1075-2617
Dixon, M.J., Andersen, O.A., van Aalten, D.M.F., Nathubhai, Amit and Eggleston, I.M. (2008) Synthesis of cyclic peptide chitinase inhibitors: Natural products with chemotherapeutic potential. Journal of Peptide Science, 14 (8). p. 13. ISSN 1075-2617
Andersen, O.A., Nathubhai, Amit, Dixon, M.J., Eggleston, I.M. and van Aalten, D.M.F. (2008) Structure-Based Dissection of the Natural Product Cyclopentapeptide Chitinase Inhibitor Argifin. Chemistry & Biology, 15 (3). pp. 295-301. ISSN 1074-5521
Dixon, M.J., Andersen, O.A., van Aalten, D. M. F., Nathubhai, Amit and Eggleston, I.M. (2007) Cyclic peptide chitinase inhibitors: New leads for antifungal and anti-inflammatory drugs. Biopolymers, 88 (4). p. 576. ISSN 0006-3525