Photo of Dr Gemma Nixon

Dr Gemma Nixon MChem, PhD

Lecturer in Medicinal Chemistry Chemistry

    Publications

    2019

    AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis (Journal article)

    Hong, W. D., Benayoud, F., Nixon, G. L., Ford, L., Johnston, K. L., Clare, R. H., . . . O'Neill, P. M. (2019). AWZ1066S, a highly specific anti-Wolbachia drug candidate for a short-course treatment of filariasis. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 116(4), 1414-1419. doi:10.1073/pnas.1816585116

    DOI: 10.1073/pnas.1816585116

    Industrial scale high-throughput screening delivers multiple fast acting macrofilaricides (Journal article)

    Clare, R. H., Bardelle, C., Harper, P., Hong, W. D., Borjesson, U., Johnston, K. L., . . . Ward, S. A. (2019). Industrial scale high-throughput screening delivers multiple fast acting macrofilaricides. NATURE COMMUNICATIONS, 10. doi:10.1038/s41467-018-07826-2

    DOI: 10.1038/s41467-018-07826-2

    2018

    Potent Antimalarial 2-Pyrazolyl Quinolone bc(1) (Q(i)) Inhibitors with Improved Drug-like Properties (Journal article)

    Hong, W. D., Leung, S. C., Amporndanai, K., Davies, J., Priestley, R. S., Nixon, G. L., . . . O'Neill, P. M. (2018). Potent Antimalarial 2-Pyrazolyl Quinolone bc(1) (Q(i)) Inhibitors with Improved Drug-like Properties. ACS MEDICINAL CHEMISTRY LETTERS, 9(12), 1205-1210. doi:10.1021/acsmedchemlett.8b00371

    DOI: 10.1021/acsmedchemlett.8b00371

    Proteolysis-targeting chimera (PROTAC) compounds to degrade S100A4 and inhibit breast cancer metastasis (Conference Paper)

    Du, M., Wang, G., Ismail, T. M., Crick, R., Barraclough, R., Daimark, B. H., . . . Rudland, P. (2018). Proteolysis-targeting chimera (PROTAC) compounds to degrade S100A4 and inhibit breast cancer metastasis. In ANNALS OF ONCOLOGY Vol. 29. Retrieved from http://gateway.webofknowledge.com/

    Repurposing and Reformulation of the Antiparasitic Agent Flubendazole for Treatment of Cryptococcal Meningoencephalitis, a Neglected Fungal Disease (Journal article)

    Nixon, G. L., McEntee, L., Johnson, A., Farrington, N., Whalley, S., Livermore, J., . . . Hope, W. (2018). Repurposing and Reformulation of the Antiparasitic Agent Flubendazole for Treatment of Cryptococcal Meningoencephalitis, a Neglected Fungal Disease. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY, 62(4). doi:10.1128/AAC.01909-17

    DOI: 10.1128/AAC.01909-17

    Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria (Journal article)

    O' Neill, P. M., Stocks, P. A., Sabbani, S., Roberts, N. L., Amewu, R. K., Shore, E. R., . . . Ward, S. A. (2018). Synthesis and profiling of benzylmorpholine 1,2,4,5-tetraoxane analogue N205: Towards tetraoxane scaffolds with potential for single dose cure of malaria. BIOORGANIC & MEDICINAL CHEMISTRY, 26(11), 2996-3005. doi:10.1016/j.bmc.2018.05.006

    DOI: 10.1016/j.bmc.2018.05.006

    2017

    A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance (Journal article)

    O'Neill, P. M., Amewu, R. K., Charman, S. A., Sabbani, S., Gnadig, N. F., Straimer, J., . . . Ward, S. A. (2017). A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance. NATURE COMMUNICATIONS, 8. doi:10.1038/ncomms15159

    DOI: 10.1038/ncomms15159

    Identification and prioritization of novel anti-Wolbachia chemotypes from screening a 10,000-compound diversity library (Journal article)

    Johnston, K. L., Cook, D. A. N., Berry, N. G., Hong, W. D., Clare, R. H., Goddard, M., . . . Taylor, M. J. (2017). Identification and prioritization of novel anti-Wolbachia chemotypes from screening a 10,000-compound diversity library. SCIENCE ADVANCES, 3(9). doi:10.1126/sciadv.aao1551

    DOI: 10.1126/sciadv.aao1551

    Rational Design, Synthesis and Biological Evaluation of Heterocyclic Quinolones Targeting the respiratory chain of Mycobacterium tuberculosis. (Journal article)

    Hong, W. D., Gibbons, P. D., Leung, S. C., Amewu, R., Stocks, P. A., Stachulski, A., . . . Nixon, G. L. (2017). Rational Design, Synthesis, and Biological Evaluation of Heterocyclic Quinolones Targeting the Respiratory Chain of Mycobacterium tuberculosis. JOURNAL OF MEDICINAL CHEMISTRY, 60(9), 3703-3726. doi:10.1021/acs.jmedchem.6b01718

    DOI: 10.1021/acs.jmedchem.6b01718

    2016

    Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action (Journal article)

    Fernandez-Alvaro, E., Hong, W. D., Nixon, G. L., O'Neil, P. M., & Calderon, F. (2016). Antimalarial Chemotherapy: Natural Product Inspired Development of Preclinical and Clinical Candidates with Diverse Mechanisms of Action. JOURNAL OF MEDICINAL CHEMISTRY, 59(12), 5587-5603. doi:10.1021/acs.jmedchem.5b01485

    DOI: 10.1021/acs.jmedchem.5b01485

    Optimisation of the synthesis of second generation 1,2,4,5 tetraoxane antimalarials (Journal article)

    O' Neill, P. M., Sabbani, S., Nixon, G. L., Schnaderbeck, M., Roberts, N. L., Shore, E. R., . . . Amewu, R. K. (2016). Optimisation of the synthesis of second generation 1,2,4,5 tetraoxane antimalarials. TETRAHEDRON, 72(40), 6118-6126. doi:10.1016/j.tet.2016.08.043

    DOI: 10.1016/j.tet.2016.08.043

    Tripodal Tris-N-oxides: Synthesis and Hydrogen Bonding Capabilities (Journal article)

    Nixon, G. L., Billington, H., Kalindjian, S. B., Steiner, A., & O'Neil, I. A. (2016). Tripodal Tris-N-oxides: Synthesis and Hydrogen Bonding Capabilities. SYNLETT, 27(1), 141-145. doi:10.1055/s-0035-1560533

    DOI: 10.1055/s-0035-1560533

    2015

    2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties (Journal article)

    Charoensutthivarakul, S., Hong, W. D., Leung, S. C., Gibbons, P. D., Bedingfield, P. T. P., Nixon, G. L., . . . O'Neill, P. M. (2015). 2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties. MEDCHEMCOMM, 6(7), 1252-1259. doi:10.1039/c5md00062a

    DOI: 10.1039/c5md00062a

    Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials (Journal article)

    McConville, M., Fernandez, J., Angulo-Barturen, I., Bahamontes-Rosa, N., Ballell-Pages, L., Castaneda, P., . . . O'Neill, P. M. (2015). Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials. JOURNAL OF MEDICINAL CHEMISTRY, 58(16), 6448-6455. doi:10.1021/acs.jmedchem.5b00434

    DOI: 10.1021/acs.jmedchem.5b00434

    Inhibitors of the Plasmodium mitochondrial respiratory chain (Chapter)

    Nixon, G., Ward, S., O'Neill, P., & Biagini, G. (2015). Inhibitors of the Plasmodium mitochondrial respiratory chain. In Encyclopedia of Malaria (pp. 1-16). Springer-Verlag Berlin Heidelberg. doi:10.1007/978-1-4614-8757-9_15-1

    DOI: 10.1007/978-1-4614-8757-9_15-1

    2013

    Antimalarial pharmacology and therapeutics of atovaquone (Journal article)

    Nixon, G. L., Moss, D. M., Shone, A. E., Lalloo, D. G., Fisher, N., O'Neill, P. M., . . . Biagini, G. A. (2013). Antimalarial pharmacology and therapeutics of atovaquone. Journal of Antimicrobial Chemotherapy, 68(5), 977-985. doi:10.1093/jac/dks504

    DOI: 10.1093/jac/dks504

    Targeting the mitochondrial electron transport chain of Plasmodium falciparum: new strategies towards the development of improved antimalarials for the elimination era (Journal article)

    Nixon, G. L., Pidathala, C., Shone, A. E., Antoine, T., Fisher, N., O'Neill, P. M., . . . Biagini, G. A. (2013). Targeting the mitochondrial electron transport chain of Plasmodium falciparum: new strategies towards the development of improved antimalarials for the elimination era. FUTURE MEDICINAL CHEMISTRY, 5(13), 1573-1591. doi:10.4155/fmc.13.121

    DOI: 10.4155/fmc.13.121

    2012

    Antimalarial pharmacology and therapeutics of atovaquone (Journal article)

    Nixon, G. L., Moss, D. M., Shone, A. E., Lalloo, D. G., Fisher, N., O'Neill, P. M., . . . Biagini, G. A. (2013). Antimalarial pharmacology and therapeutics of atovaquone. JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 68(5), 977-985. doi:10.1093/jac/dks504

    DOI: 10.1093/jac/dks504

    Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria (Journal article)

    Biagini, G. A., Fisher, N., Shone, A. E., Mubaraki, M. A., Srivastava, A., Hill, A., . . . Ward, S. A. (2012). Generation of quinolone antimalarials targeting the Plasmodium falciparum mitochondrial respiratory chain for the treatment and prophylaxis of malaria. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 109(21), 8298-8303. doi:10.1073/pnas.1205651109

    DOI: 10.1073/pnas.1205651109

    Identification of Novel Antimalarial Chemotypes via Chemoinformatic Compound Selection Methods for a High-Throughput Screening Program against the Novel Malarial Target, PfNDH2: Increasing Hit Rate via Virtual Screening Methods (Journal article)

    Sharma, R., Lawrenson, A. S., Fisher, N. E., Warman, A. J., Shone, A. E., Hill, A., . . . Berry, N. G. (2012). Identification of Novel Antimalarial Chemotypes via Chemoinformatic Compound Selection Methods for a High-Throughput Screening Program against the Novel Malarial Target, PfNDH2: Increasing Hit Rate via Virtual Screening Methods. JOURNAL OF MEDICINAL CHEMISTRY, 55(7), 3144-3154. doi:10.1021/jm3001482

    DOI: 10.1021/jm3001482

    Identification, Design and Biological Evaluation of Bisaryl Quinolones Targeting Plasmodium falciparum Type II NADH:Quinone Oxidoreductase (PfNDH2) (Journal article)

    Pidathala, C., Amewu, R., Pacorel, B., Nixon, G. L., Gibbons, P., Hong, W. D., . . . O'Neill, P. M. (2012). Identification, Design and Biological Evaluation of Bisaryl Quinolones Targeting Plasmodium falciparum Type II NADH:Quinone Oxidoreductase (PfNDH2). JOURNAL OF MEDICINAL CHEMISTRY, 55(5), 1831-1843. doi:10.1021/jm201179h

    DOI: 10.1021/jm201179h

    Identification, Design and Biological Evaluation of Heterocyclic Quinolones Targeting Plasmodium falciparum Type II NADH:Quinone Oxidoreductase (PfNDH2) (Journal article)

    Leung, S. C., Gibbons, P., Amewu, R., Nixon, G. L., Pidathala, C., Hong, W. D., . . . O'Neill, P. M. (2012). Identification, Design and Biological Evaluation of Heterocyclic Quinolones Targeting Plasmodium falciparum Type II NADH:Quinone Oxidoreductase (PfNDH2). JOURNAL OF MEDICINAL CHEMISTRY, 55(5), 1844-1857. doi:10.1021/jm201184h

    DOI: 10.1021/jm201184h

    2010

    A novel drug for uncomplicated malaria: Targeted high throughput screening (HTS) against the type II NADH:ubiquinone oxidoreductase (PfNDH2) of Plasmodium falciparum (Journal article)

    Fisher, N., Hill, A., Mbekeani, A., Shone, A., Nixon, G., Stocks, P., . . . Biagini, G. A. (2010). A novel drug for uncomplicated malaria: Targeted high throughput screening (HTS) against the type II NADH:ubiquinone oxidoreductase (PfNDH2) of Plasmodium falciparum. BIOCHIMICA ET BIOPHYSICA ACTA-BIOENERGETICS, 1797, 80. doi:10.1016/j.bbabio.2010.04.241

    DOI: 10.1016/j.bbabio.2010.04.241

    Development of a novel drug for uncomplicated malaria targeting the mitochondrial NADH:quinone oxidoreductase (Journal article)

    Biagini, G. A., Hill, A., Mbekeani, A., Shone, A., Nixon, G., Stocks, P., . . . Ward, S. A. (2010). Development of a novel drug for uncomplicated malaria targeting the mitochondrial NADH:quinone oxidoreductase. Malaria Journal, 9(Suppl 2), O4. doi:10.1186/1475-2875-9-S2-O4

    DOI: 10.1186/1475-2875-9-S2-O4

    Endoperoxide Carbonyl Falcipain 2/3 Inhibitor Hybrids: Toward Combination Chemotherapy of Malaria through a Single Chemical Entity (Journal article)

    Gibbons, P., Verissimo, E., Araujo, N. C., Barton, V., Nixon, G. L., Amewu, R. K., . . . O'Neill, P. M. (2010). Endoperoxide Carbonyl Falcipain 2/3 Inhibitor Hybrids: Toward Combination Chemotherapy of Malaria through a Single Chemical Entity. JOURNAL OF MEDICINAL CHEMISTRY, 53(22), 8202-8206. doi:10.1021/jm1009567

    DOI: 10.1021/jm1009567

    Identification of a 1,2,4,5-Tetraoxane Antimalarial Drug-Development Candidate (RKA 182) with Superior Properties to the Semisynthetic Artemisinins (Journal article)

    O'Neill, P. M., Amewu, R. K., Nixon, G. L., ElGarah, F. B., Mungthin, M., Chadwick, J., . . . Ward, S. A. (2010). Identification of a 1,2,4,5-Tetraoxane Antimalarial Drug-Development Candidate (RKA 182) with Superior Properties to the Semisynthetic Artemisinins. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 49(33), 5693-5697. doi:10.1002/anie.201001026

    DOI: 10.1002/anie.201001026

    Synthesis, in vitro and in vivo antimalarial assessment of sulfide, sulfone and vinyl amide-substituted 1,2,4-trioxanes prepared via thiol-olefin co-oxygenation (TOCO) of allylic alcohols (Journal article)

    Amewu, R., Gibbons, P., Mukhtar, A., Stachulski, A. V., Ward, S. A., Hall, C., . . . O'Neill, P. M. (2010). Synthesis, in vitro and in vivo antimalarial assessment of sulfide, sulfone and vinyl amide-substituted 1,2,4-trioxanes prepared via thiol-olefin co-oxygenation (TOCO) of allylic alcohols. ORGANIC & BIOMOLECULAR CHEMISTRY, 8(9), 2068-2077. doi:10.1039/b924319d

    DOI: 10.1039/b924319d

    2009

    Synthesis, Antimalarial Activity, and Preclinical Pharmacology of a Novel Series of 4 '-Fluoro and 4 '-Chloro Analogues of Amodiaquine. Identification of a Suitable "Back-Up" Compound for N-tert-Butyl Isoquine (Journal article)

    O'Neill, P. M., Shone, A. E., Stanford, D., Nixon, G., Asadollahy, E., Park, B. K., . . . Ward, S. A. (2009). Synthesis, Antimalarial Activity, and Preclinical Pharmacology of a Novel Series of 4 '-Fluoro and 4 '-Chloro Analogues of Amodiaquine. Identification of a Suitable "Back-Up" Compound for N-tert-Butyl Isoquine. JOURNAL OF MEDICINAL CHEMISTRY, 52(7), 1828-1844. doi:10.1021/jm8012757

    DOI: 10.1021/jm8012757

    2008

    An efficient route into synthetically challenging bridged achiral 1,2,4,5-tetraoxanes with antimalarial activity (Journal article)

    Ellis, G. L., Amewu, R., Hall, C., Rimmer, K., Ward, S. A., & O'Neill, P. M. (2008). An efficient route into synthetically challenging bridged achiral 1,2,4,5-tetraoxanes with antimalarial activity. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 18(5), 1720-1724. doi:10.1016/j.bmcl.2008.01.053

    DOI: 10.1016/j.bmcl.2008.01.053

    An efficient route into synthetically challenging bridged achiral 1,2,4,5-tetraoxanes with antimalarial activity (Journal article)

    Ellis, G. L., Amewu, R., Hall, C., Rimmer, K., Ward, S. A., & O’Neill, P. M. (2008). An efficient route into synthetically challenging bridged achiral 1,2,4,5-tetraoxanes with antimalarial activity. Bioorganic & Medicinal Chemistry Letters, 18(5), 1720-1724. doi:10.1016/j.bmcl.2008.01.053

    DOI: 10.1016/j.bmcl.2008.01.053

    Piperidine dispiro-1,2,4-trioxane analogues (Journal article)

    Sabbani, S., Stocks, P. A., Ellis, G. L., Davies, J., Hedenstrom, E., Ward, S. A., & O'Neill, P. M. (2008). Piperidine dispiro-1,2,4-trioxane analogues. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 18(21), 5804-5808. doi:10.1016/j.bmcl.2008.09.052

    DOI: 10.1016/j.bmcl.2008.09.052

    Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles (Journal article)

    Ellis, G. L., Amewu, R., Sabbani, S., Stocks, P. A., Shone, A., Stanford, D., . . . O'Neill, P. M. (2008). Two-step synthesis of achiral dispiro-1,2,4,5-tetraoxanes with outstanding antimalarial activity, low toxicity, and high-stability profiles. JOURNAL OF MEDICINAL CHEMISTRY, 51(7), 2170-2177. doi:10.1021/jm701435h

    DOI: 10.1021/jm701435h

    2007

    Evidence for a Common Non-Heme Chelatable-Iron-Dependent Activation Mechanism for Semisynthetic and Synthetic Endoperoxide Antimalarial Drugs (Journal article)

    Stocks, P. A., Bray, P. G., Barton, V., Al-Helal, M., Jones, M., Araujo, N. C., . . . O'Neill, P. (2007). Evidence for a Common Non-Heme Chelatable-Iron-Dependent Activation Mechanism for Semisynthetic and Synthetic Endoperoxide Antimalarial Drugs. Angewandte Chemie International Edition, 46(33), 6278-6283. doi:10.1002/anie.200604697

    DOI: 10.1002/anie.200604697

    Evidence for a common non-heme chelatable-iron-dependent activation mechanism for semisynthetic and synthetic endoperoxide antimalarial drugs (Journal article)

    Stocks, P. A., Bray, P. G., Barton, V. E., Al-Helal, M., Jones, M., Araujo, N. C., . . . O'Neill, P. M. (2007). Evidence for a common non-heme chelatable-iron-dependent activation mechanism for semisynthetic and synthetic endoperoxide antimalarial drugs. ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, 46(33), 6278-6283. doi:10.1002/anie.200604697

    DOI: 10.1002/anie.200604697

    The diastereoselective synthesis of functionalised spirocyclic lactams and lactones using a Cope elimination/intramolecular nitrone cycloaddition strategy (Journal article)

    Ellis, G. L., O'Neil, I. A., Ramos, V. E., Kalindjian, S. B., Chorlton, A. P., & Tapolczay, D. J. (2007). The diastereoselective synthesis of functionalised spirocyclic lactams and lactones using a Cope elimination/intramolecular nitrone cycloaddition strategy. TETRAHEDRON LETTERS, 48(10), 1687-1690. doi:10.1016/j.tetlet.2007.01.046

    DOI: 10.1016/j.tetlet.2007.01.046

    The diastereoselective synthesis of functionalised spirocyclic lactams and lactones using a Cope elimination/intramolecular nitrone cycloaddition strategy (Journal article)

    Ellis, G. L., O’Neil, I. A., Ramos, V. E., Kalindjian, S. B., Chorlton, A. P., & Tapolczay, D. J. (2007). The diastereoselective synthesis of functionalised spirocyclic lactams and lactones using a Cope elimination/intramolecular nitrone cycloaddition strategy. Tetrahedron Letters, 48(10), 1687-1690. doi:10.1016/j.tetlet.2007.01.046

    DOI: 10.1016/j.tetlet.2007.01.046

    The synthesis of functionalised chiral bicyclic lactam and lactone N-oxides using a tandem Cope elimination/reverse Cope elimination protocol (Journal article)

    Ellis, G. L., O'Neil, I. A., Ramos, V. E., Cleator, E., Kalindjian, S. B., Chorlton, A. P., & Tapolczay, D. J. (2007). The synthesis of functionalised chiral bicyclic lactam and lactone N-oxides using a tandem Cope elimination/reverse Cope elimination protocol. TETRAHEDRON LETTERS, 48(10), 1683-1686. doi:10.1016/j.tetlet.2007.01.045

    DOI: 10.1016/j.tetlet.2007.01.045

    2004

    The diastereoselective synthesis of functionalised isoxazolidines using a Cope elimination/intramolecular nitrone cycloaddition strategy (Journal article)

    O'Neil, I. A., Ramos, V., Ellis, G. L., Cleator, E., Chorlton, A. P., Tapolczay, D. J., & Kalindjian, S. (2004). The diastereoselective synthesis of functionalised isoxazolidines using a Cope elimination/intramolecular nitrone cycloaddition strategy. Tetrahedron Letters, 45(18), 3659-3661. doi:10.1016/j.tetlet.2004.03.041

    DOI: 10.1016/j.tetlet.2004.03.041

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