Tisnerat, Camille, Di Ciano, Samuele, Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101 and Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910
2025.
Microwave-accelerated synthesis of novel triphosphate nucleoside prodrugs: Expanding the therapeutic arsenal of anticancer agents.
Organic Letters
27
(1)
, pp. 322-327.
10.1021/acs.orglett.4c04379
|
|
|
Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Morozzi, Chiara, James, Edward, Renno, Giacomo, Cardano, Francesca and Fin, Andrea
2024.
Fingolimod phosphoramidate prodrugs: Synthesis, photophysical characterisation and lipid bilayer interaction of fluorescent tagged Prodrug.
Journal of Molecular Structure
1312
(2)
, 138614.
10.1016/j.molstruc.2024.138614
|
|
|
Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, di Ciano, Samule and Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101
2024.
Design, synthesis and biological evaluation of aryloxy thiophosphoramidate triesters of anticancer nucleoside analogues.
Bioorganic and Medicinal Chemistry
103
, 117696.
10.1016/j.bmc.2024.117696
|
|
|
Douglas, EdwardJ. A., Marshall, Brandon, Alghamadi, Arwa, Joseph, Erin A., Duggan, Seána, Vittorio, Serena, De Luca, Laura, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910 and Laabei, Maisem
2023.
Improved antibacterial activity of 1,3,4-oxadiazole-based compounds that restrict Staphylococcus aureus growth independent of LtaS function.
ACS Infectious Diseases
9
(11)
, pp. 2141-2159.
10.1021/acsinfecdis.3c00250
|
|
|
Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, Morozzi, Chiara, Novelli, Giulia, Giannantonio, Daniele, Duggan, Katrina, Vittorio, Serena, Fallis, Ian A. ORCID: https://orcid.org/0000-0001-7361-0182, De Luca, Laura and Williams, David ORCID: https://orcid.org/0000-0002-7351-5131
2023.
Synthesis, molecular docking and antibacterial activity of an oxadiazole-based lipoteichoic acid inhibitor and its metabolites.
Journal of Molecular Structure
1278
, 134977.
10.1016/j.molstruc.2023.134977
|
|
|
Cook, Sophie R., Kirkham, Emily D., Best, Hannah, Waller-Evans, Helen ORCID: https://orcid.org/0000-0003-4133-6064, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101 and Lloyd-Evans, Emyr ORCID: https://orcid.org/0000-0002-3626-1611
2023.
Investigating lysosomal and cellular phenotypes of the lysosomal disorder cystinosis.
Presented at: 19th Annual WORLDSymposium™ 2023,
Orlando, Florida,
21-26 February 2023.
Molecular Genetics and Metabolism.
, vol.138
(2)
Elsevier,
p. 28.
10.1016/j.ymgme.2022.107061
|
|
Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Ferrari, Valentina ORCID: https://orcid.org/0000-0003-1895-8906, McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X, Ghazaly, Essam and Pepper, Chris
2022.
Synthesis and characterization of nuc-7738, an aryloxy phosphoramidate of 3?-deoxyadenosine, as a potential anticancer agent.
Journal of Medicinal Chemistry
65
(23)
, pp. 15789-15804.
10.1021/acs.jmedchem.2c01348
|
|
|
Schwenzer, Hagen, De Zan, Erica, Elshani, Mustafa, van Stiphout, Ruud, Kudsy, Mary, Morris, Josephine, Ferrari, Valentina ORCID: https://orcid.org/0000-0003-1895-8906, Um, In Hwa, Chettle, James, Kazmi, Farasat, Campo, Leticia, Easton, Alistair, Nijman, Sebastian, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Symeonides, Stefan, Plummer, Ruth, Harrison, David J., Bond, Gareth and Blagden, Sarah P.
2021.
The novel nucleoside analogue ProTide NUC-7738 overcomes cancer resistance mechanisms in vitro and in a first-in-human Phase 1 clinical trial.
Clinical Cancer Research
27
(23)
, pp. 6500-6513.
10.1158/1078-0432.CCR-21-1652
|
|
|
Slusarczyk, Magdalena ORCID: https://orcid.org/0000-0002-4707-7190, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Ghazaly, Essam, Kariuki, Benson M. ORCID: https://orcid.org/0000-0002-8658-3897, McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X and Pepper, Chris
2021.
Single diastereomers of the clinical anticancer ProTide agents NUC-1031 and NUC-3373 preferentially target cancer stem cells in vitro.
Journal of Medicinal Chemistry
64
(12)
, pp. 8179-8193.
10.1021/acs.jmedchem.0c02194
|
|
|
| NuCana PLC 2021. Phosphoramidate nucleoside derivatives as anticancer agents. WO2017207986A1; US20210130387A1. [Patent]. |
|
Vanden Avond, Mark A., Meng, Hui, Beatka, Margaret J., Helbling, Daniel C., Prom, Mariah J., Sutton, Jessica L., Slick, Rebecca A., Dimmock, David P., Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Pileggi, Elisa, Crutcher, Patrick, Thomas, Stephen and Lawlor, Michael W.
2021.
The nucleotide prodrug CERC‐913 improves mtDNA content in primary hepatocytes from DGUOK‐deficient rats.
Journal of Inherited Metabolic Disease
44
(2)
, pp. 492-501.
10.1002/jimd.12354
|
|
|
Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910 and Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101
2021.
An overview of ProTide technology and its implications to drug discovery.
Expert Opinion on Drug Discovery
16
(10)
, 1149--1161.
10.1080/17460441.2021.1922385
|
|
|
Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, Pileggi, Elisa, Richards, Jennifer, Wootton, Mandy, Van Leemputte, Thijs, Persoons, Leentje, De Coster, David, Villanueva, Xabier, Daelemans, Dirk, Steenackers, Hans, McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X and Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910
2020.
Drug repurposing: phosphate prodrugs of anticancer and antiviral FDA-approved nucleosides as novel antimicrobials.
Journal of Antimicrobial Chemotherapy
75
(10)
, pp. 2864-2878.
10.1093/jac/dkaa268
|
|
|
Morozzi, Chiara, Sedláková, Jana, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Avigliano, Marialuce, Carbajo, Rosangela, Sandoval, Lucia, Valles-Ayoub, Yadira, Crutcher, Patrick, Thomas, Stephen and Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101
2019.
Targeting GNE myopathy: A dual prodrug approach for the delivery of N-acetylmannosamine 6-phosphate.
Journal of Medicinal Chemistry
62
(17)
, pp. 8178-8193.
10.1021/acs.jmedchem.9b00833
|
|
|
Slusarczyk, Magdalena ORCID: https://orcid.org/0000-0002-4707-7190, Ferrari, Valentina ORCID: https://orcid.org/0000-0003-1895-8906, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Gonczy, Blanka, Balzarini, Jan and McGuigan, Christopher
2018.
Symmetrical diamidates as a class of phosphate prodrugs to deliver the 5'-monophosphate form of anticancer nucleoside analogues.
ChemMedChem
13
(21)
, pp. 2305-2316.
10.1002/cmdc.201800504
|
|
|
Pileggi, Elisa, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910 and Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101
2018.
Preparation of pyrimidine alkenyl acyclic nucleoside phosphonoamidates.
Current Protocols in Nucleic Acid Chemistry
74
(13-14)
, e56.
10.1002/cpnc.56
|
|
|
Pileggi, Elisa, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Andrei, Graciela, Schols, Dominique, Snoeck, Robert and Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101
2018.
Expedient synthesis and biological evaluation of alkenyl acyclic nucleoside phosphonate prodrugs.
Bioorganic and Medicinal Chemistry
26
(12)
, pp. 3596-3609.
10.1016/j.bmc.2018.05.034
|
|
|
| NuCana Biomed Ltd 2017. Adenosine derivatives for use in the treatment of cancer. WO2017207989A1. [Patent]. |
|
Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, De Biasi, Roberto, Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, Slusarczyk, Magdalena ORCID: https://orcid.org/0000-0002-4707-7190 and McGuigan, Christopher
2017.
Synthetic approaches for the preparation of phosphoramidate prodrugs of 2’-deoxypseudoisocytidine.
ChemistryOpen
6
(3)
, pp. 424-436.
10.1002/open.201700019
|
|
|
Marinozzi, Maura, Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101 and Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910
2016.
λ5-Phosphorus-Containing α-Diazo Compounds (PCDCs): a valuable tool for accessing phosphorus-functionalized molecules.
Chemical Reviews
116
(22)
, pp. 13991-14055.
10.1021/acs.chemrev.6b00373
|
|
|
Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Ferrari, Valentina and Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101
2016.
Nucleosided derived antibiotics to fight microbial drug resistance: New utilities for an established class of drugs?
Journal of Medicinal Chemistry
59
(23)
, pp. 10343-10382.
10.1021/acs.jmedchem.6b00325
|
|
|
McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Slusarczyk, Magdalena ORCID: https://orcid.org/0000-0002-4707-7190, Ferrari, Valentina ORCID: https://orcid.org/0000-0003-1895-8906, Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, Meneghesso, Silvia, Derudas, Marco, Farleigh, Laura, Zanetta, Paola and Bugert, Joachim ORCID: https://orcid.org/0000-0002-0556-3211
2016.
Anti-flavivirus activity of different tritylated pyrimidine and purine nucleoside analogues.
ChemistryOpen
5
(3)
, pp. 227-235.
10.1002/open.201500216
|
|
|
Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X and Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910
2015.
Symmetrical diamidate prodrugs of nucleotide analogues for drug delivery.
Current Protocols in Nucleic Acid Chemistry,
Wiley-Blackwell,
60:15.6.1-15.6.10.
(10.1002/0471142700.nc1506s60)
|
|
|
| NuCana PLC 2015. Gemcitabine Prodrugs. WO 2015/198058; GB51857. [Patent]. |
|
Ferrari, Valentina ORCID: https://orcid.org/0000-0003-1895-8906, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X and Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101
2015.
Chemoselective N-deacetylation of protected nucleosides and nucleotides promoted by the Schwartz's reagent.
Nucleosides, Nucleotides & Nucleic Acids
34
(11)
, pp. 799-814.
10.1080/15257770.2015.1075552
|
|
|
Ferrari, Valentina ORCID: https://orcid.org/0000-0003-1895-8906 and Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910
2015.
Nucleoside analogs and tuberculosis: new weapons against an old enemy.
Future Medicinal Chemistry
7
(3)
, pp. 291-314.
10.4155/fmc.14.166
|
|
|
McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X, Derudas, Marco, Gonczy, Blanka, Hinsinger, Karen, Kandil, Sahar ORCID: https://orcid.org/0000-0003-1806-9623, Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Snoeck, Robert, Andrei, Graciela, Balzarini, Jan, McHugh, Timothy D., Maitra, Arundhati, Akorli, Ernest, Evangelopoulos, Dimitrios and Bhakta, Sanjib
2014.
ProTides of N-(3-(5-(2'-deoxyuridine))prop-2-ynyl)octanamide as potential anti-tubercular and anti-viral agents.
Bioorganic and Medicinal Chemistry
22
(9)
, pp. 2816-2824.
10.1016/j.bmc.2014.02.056
|
|
|
| Magdalena Slusarczyk 2014. Prodrug. IN 2014MU02050. [Patent]. |
|
McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X, Bourdin, Claire, Derudas, Marco, Hamon, Nadege, Hinsinger, Karen, Kandil, Sahar ORCID: https://orcid.org/0000-0003-1806-9623, Madela, Karolina, Meneghesso, Silvia, Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Slusarczyk, Magdalena ORCID: https://orcid.org/0000-0002-4707-7190, Chamberlain, Stanley, Kolykhalov, Alexander, Vernachio, John, Vanpouille, Christophe, Introini, Andrea, Margolis, Leonid and Balzarini, Jan
2013.
Design, synthesis and biological evaluation of phosphorodiamidate prodrugs of antiviral and anticancer nucleosides.
European Journal of Medicinal Chemistry
70
, pp. 326-340.
10.1016/j.ejmech.2013.09.047
|
|
|
Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Bibbo, Rita, Rat, Stephanie, Roberts, Helen Christina, Hughes, Clare Elizabeth ORCID: https://orcid.org/0000-0003-4726-5877, Caterson, Bruce ORCID: https://orcid.org/0000-0001-6016-0661, Alcaraz, María José, Gibert, Anna Torrent, Verson, Carlos Raul Alaez and McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X
2012.
Novel phosphoramidate prodrugs of N-Acetyl-(d)-Glucosamine with antidegenerative activity on bovine and human cartilage explants.
Journal of Medicinal Chemistry
55
(10)
, pp. 4629-4639.
10.1021/jm300074y
|
|
Pertusati, Fabrizio ORCID: https://orcid.org/0000-0003-4532-9101, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910 and McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X
2011.
Medicinal chemistry of nucleoside phosphonate prodrugs for antiviral therapy.
Antiviral Chemistry and Chemotherapy
22
(5)
, pp. 181-203.
10.3851/IMP2012
|
|
|
Morgan, Alwena Haf, Hammond, Victoria Jayne, Morgan, Lloyd, Thomas, Christopher P. ORCID: https://orcid.org/0000-0001-5840-8613, Tallman, Keri A., Garcia-Diaz, Yoel Ruslan, McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Porter, Ned A., Murphy, Robert C. and O'Donnell, Valerie Bridget ORCID: https://orcid.org/0000-0003-4089-8460
2010.
Quantitative assays for esterified oxylipins generated by immune cells.
Nature Protocols
5
(12)
, pp. 1919-1931.
10.1038/nprot.2010.162
|
|
McGuigan, Christopher ORCID: https://orcid.org/0000-0001-8409-710X, Serpi, Michaela ORCID: https://orcid.org/0000-0002-6162-7910, Bibbo, Rita, Roberts, Helen Christina, Hughes, Clare Elizabeth ORCID: https://orcid.org/0000-0003-4726-5877, Caterson, Bruce ORCID: https://orcid.org/0000-0001-6016-0661, Gibert, Ana Torrent and Verson, Carlos Raul Alaez
2008.
Phosphate prodrugs derived from N-acetylglucosamine have enhanced chondroprotective activity in explant cultures and represent a new lead in antiosteoarthritis drug discovery.
Journal of Medicinal Chemistry
51
(18)
, pp. 5807-5812.
10.1021/jm800594c
|
|



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