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Gemma Nixon

Dr Gemma Nixon
MChem, PhD

Senior Lecturer in Medicinal Chemistry
Chemistry

Publications

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2024

Design, synthesis and modelling of photoreactive chemical probes for investigating target engagement of plasmepsin IX and X in <i>Plasmodium falciparum</i>.

Lisauskaitė, M., Nixon, G. L., Woodley, C. M., Berry, N. G., Coninckx, A., Qie, L. C., . . . O'Neill, P. M. (2024). Design, synthesis and modelling of photoreactive chemical probes for investigating target engagement of plasmepsin IX and X in <i>Plasmodium falciparum</i>.. RSC chemical biology, 5(1), 19-29. doi:10.1039/d3cb00109a

DOI
10.1039/d3cb00109a
Journal article

2023

Identification of 2-Aryl-Quinolone Inhibitors of Cytochrome bd and Chemical Validation of Combination Strategies for Respiratory Inhibitors against Mycobacterium tuberculosis

Jeffreys, L. N., Ardrey, A., Hafiz, T. A., Dyer, L. -A., Warman, A. J., Mosallam, N., . . . Biagini, G. A. (2023). Identification of 2-Aryl-Quinolone Inhibitors of Cytochrome bd and Chemical Validation of Combination Strategies for Respiratory Inhibitors against Mycobacterium tuberculosis. ACS INFECTIOUS DISEASES. doi:10.1021/acsinfecdis.2c00283

DOI
10.1021/acsinfecdis.2c00283
Journal article

2021

Therapeutic Potential of Nitazoxanide: An Appropriate Choice for Repurposing versus SARS-CoV-2?

Stachulski, A. V., Taujanskas, J., Pate, S. L., Rajoli, R. K. R., Aljayyoussi, G., Pennington, S. H., . . . O'Neill, P. M. (2021). Therapeutic Potential of Nitazoxanide: An Appropriate Choice for Repurposing versus SARS-CoV-2?. ACS INFECTIOUS DISEASES, 7(6), 1317-1331. doi:10.1021/acsinfecdis.0c00478

DOI
10.1021/acsinfecdis.0c00478
Journal article

2019

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

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
Journal article

2018

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

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 https://www.webofscience.com/

Conference Paper

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

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
Journal article

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

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), e01909-e01917. doi:10.1128/aac.01909-17

DOI
10.1128/aac.01909-17
Journal article

2017

A tetraoxane-based antimalarial drug candidate that overcomes PfK13-C580Y dependent artemisinin resistance

O'Neill, P. M., Amewu, R. K., Charman, S. A., Sabbani, S., Gnädig, 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
Journal article

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

Hong, W. D., Gibbons, P. D., Leung, S. C., Amewu, R., Stocks, P. A., Stachulski, A. V., . . . 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
Journal article

2016

Tripodal Tris-N-oxides: Synthesis and Hydrogen Bonding Capabilities

Nixon, G., Billington, H., Kalindjian, S., Steiner, A., & O'Neil, I. (2016). Tripodal Tris-N-oxides: Synthesis and Hydrogen Bonding Capabilities. Synlett, 27(01), 141-145. doi:10.1055/s-0035-1560533

DOI
10.1055/s-0035-1560533
Journal article

2015

Carbamoyl triazoles, Known Serine Protease Inhibitors, are a potent New Class of Antimalarial

O'Neill, P., McConville, M., Fernandez-molina, J., Angulo-Barturen, I., Bahamontes, N. R., Ballell-Pages, L., . . . Calderon, F. (2015). Carbamoyl triazoles, Known Serine Protease Inhibitors, are a potent New Class of Antimalarial. Journal of Medicinal Chemistry, 58(16), 6448-6455. doi:10.1021/acs.jmedchem.5b00434

DOI
10.1021/acs.jmedchem.5b00434
Journal article

2-Pyridylquinolone antimalarials with improved antimalarial activity and physicochemical properties

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
Journal article

Inhibitors of the Plasmodium Mitochondrial Respiratory Chain

Nixon, G. L., Ward, S. A., O’Neill, P. M., & Biagini, G. A. (2014). Inhibitors of the Plasmodium Mitochondrial Respiratory Chain. In Encyclopedia of Malaria (pp. 1-18). Springer New York. doi:10.1007/978-1-4614-8757-9_15-1

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

2013

Targeting the mitochondrial electron transport chain of <i>Plasmodium falciparum</i>: new strategies towards the development of improved antimalarials for the elimination era

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 <i>Plasmodium falciparum</i>: new strategies towards the development of improved antimalarials for the elimination era. FUTURE MEDICINAL CHEMISTRY, 5(13), 1573-1591. doi:10.4155/fmc.13.180

DOI
10.4155/fmc.13.180
Journal article

Antimalarial pharmacology and therapeutics of atovaquone

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
Journal article

2012

Generation of quinolone antimalarials targeting the <i>Plasmodium falciparum</i> mitochondrial respiratory chain for the treatment and prophylaxis of malaria

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 <i>Plasmodium falciparum</i> 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
Journal article

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

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
Journal article

Identification, Design and Biological Evaluation of Bisaryl Quinolones Targeting <i>Plasmodium falciparum</i> Type II NADH:Quinone Oxidoreductase (PfNDH2)

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 <i>Plasmodium falciparum</i> Type II NADH:Quinone Oxidoreductase (PfNDH2). JOURNAL OF MEDICINAL CHEMISTRY, 55(5), 1831-1843. doi:10.1021/jm201179h

DOI
10.1021/jm201179h
Journal article

Identification, Design and Biological Evaluation of Heterocyclic Quinolones Targeting <i>Plasmodium falciparum</i> Type II NADH:Quinone Oxidoreductase (PfNDH2)

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 <i>Plasmodium falciparum</i> Type II NADH:Quinone Oxidoreductase (PfNDH2). JOURNAL OF MEDICINAL CHEMISTRY, 55(5), 1844-1857. doi:10.1021/jm201184h

DOI
10.1021/jm201184h
Journal article

2010

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

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
Journal article

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

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
Journal article

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

O'Neill, P. M., Amewu, R. K., Nixon, G. L., Bousejra ElGarah, F., 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, 122(33), 5829-5833. doi:10.1002/ange.201001026

DOI
10.1002/ange.201001026
Journal article

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

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 <i>Plasmodium falciparum</i>. BIOCHIMICA ET BIOPHYSICA ACTA-BIOENERGETICS, 1797, 80. doi:10.1016/j.bbabio.2010.04.241

DOI
10.1016/j.bbabio.2010.04.241
Journal article

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

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

DOI
10.1039/b924319d
Journal article

A novel drug for uncomplicated malaria: targeted high throughput screening (HTS) against the type II NADH:ubiquinone oxidoreductase (PfNdh2) of Plasmodium falciparum

Ward, S. A., Fisher, N., Hill, A., Mbekeani, A., Shone, A., Nixon, G., . . . 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. Malaria journal, 9(Suppl 2), I14. doi:10.1186/1475-2875-9-s2-i14

DOI
10.1186/1475-2875-9-s2-i14
Journal article

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 <i>N-tert</i>-Butyl Isoquine

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 <i>N-tert</i>-Butyl Isoquine. JOURNAL OF MEDICINAL CHEMISTRY, 52(7), 1828-1844. doi:10.1021/jm8012757

DOI
10.1021/jm8012757
Journal article

ChemInform Abstract: Piperidine Dispiro‐1,2,4‐trioxane Analogues.

Sabbani, S., Stocks, P. A., Ellis, G. L., Davies, J., Hedenstrom, E., Ward, S. A., & O'Neill, P. M. (2009). ChemInform Abstract: Piperidine Dispiro‐1,2,4‐trioxane Analogues.. ChemInform, 40(9). doi:10.1002/chin.200909168

DOI
10.1002/chin.200909168
Journal article

2008

Piperidine dispiro-1,2,4-trioxane analogues

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
Journal article

ChemInform Abstract: An Efficient Route into Synthetically Challenging Bridged Achiral 1,2,4,5‐Tetraoxanes with Antimalarial Activity.

Ellis, G. L., Amewu, R., Hall, C., Rimmer, K., Ward, S. A., & O'Neill, P. M. (2008). ChemInform Abstract: An Efficient Route into Synthetically Challenging Bridged Achiral 1,2,4,5‐Tetraoxanes with Antimalarial Activity.. ChemInform, 39(37). doi:10.1002/chin.200837161

DOI
10.1002/chin.200837161
Journal article

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

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
Journal article

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

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
Journal article

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

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 &amp; Medicinal Chemistry Letters, 18(5), 1720-1724. doi:10.1016/j.bmcl.2008.01.053

DOI
10.1016/j.bmcl.2008.01.053
Journal article

2007

Evidence for a Common Non‐Heme Chelatable‐Iron‐Dependent Activation Mechanism for Semisynthetic and Synthetic Endoperoxide Antimalarial Drugs

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, 119(33), 6394-6399. doi:10.1002/ange.200604697

DOI
10.1002/ange.200604697
Journal article

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

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
Journal article

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

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
Journal article

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

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
Journal article

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

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
Journal article

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

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
Journal article

2004

The Diastereoselective Synthesis of Functionalized Isoxazolidines Using a Cope Elimination/Intramolecular Nitrone Cycloaddition Strategy.

O'Neil, I. A., Ramos, V. E., Ellis, G. L., Cleator, E., Chorlton, A. P., Tapolczay, D. J., & Kalindjian, S. B. (2004). The Diastereoselective Synthesis of Functionalized Isoxazolidines Using a Cope Elimination/Intramolecular Nitrone Cycloaddition Strategy.. ChemInform, 35(33). doi:10.1002/chin.200433148

DOI
10.1002/chin.200433148
Journal article

The diastereoselective synthesis of functionalised isoxazolidines using a Cope elimination/intramolecular nitrone cycloaddition strategy

O'Neil, I. A., Ramos, V. E., Ellis, G. L., Cleator, E., Chorlton, A. P., Tapolczay, D. J., & Kalindjian, S. B. (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
Journal article