Dr Fabrizio Pertusati

2023

• Serpi, M. et al. 2023. Synthesis, molecular docking and antibacterial activity of an oxadiazole-based lipoteichoic acid inhibitor and its metabolites. Journal of Molecular Structure 1278, article number: 134977. (10.1016/j.molstruc.2023.134977)

2022

• Pertusati, F. and Morewood, J. 2022. Synthesis of 2‐Acetamido‐1,3,4‐Tri‐O‐Acetyl‐2‐Deoxy‐D‐Mannopyranose ‐6‐Phosphate Prodrugs as potential therapeutic agents. Current Protocols 2(8), article number: e500. (10.1002/cpz1.500)

2021

• Vanden Avond, M. A. et al. 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, M. and Pertusati, F. 2021. An overview of ProTide technology and its implications to drug discovery. Expert Opinion on Drug Discovery 16(10), pp. 1149--1161. (10.1080/17460441.2021.1922385)

2020

• Pertusati, F. et al. 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)

2019

• Pertusati, F., Ferla, S., Bassetto, M., Brancale, A., Kandil, S., Westwell, A. D. and McGuigan, C. 2019. A new series of bicalutamide, enzalutamide and enobosarm derivatives carrying pentafluorosulfanyl (SF5) and pentafluoroethyl (C2F5) substituents: Improved antiproliferative agents against prostate cancer. European Journal of Medicinal Chemistry 180, pp. 1-14. (10.1016/j.ejmech.2019.07.001)
• Morozzi, C. et al. 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)

2018

• Pileggi, E., Serpi, M. and Pertusati, F. 2018. Preparation of pyrimidine alkenyl acyclic nucleoside phosphonoamidates. Current Protocols in Nucleic Acid Chemistry 74(13-14), article number: e56. (10.1002/cpnc.56)
• Pileggi, E., Serpi, M., Andrei, G., Schols, D., Snoeck, R. and Pertusati, F. 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)
• Slusarczyk, M., Serpi, M. and Pertusati, F. 2018. Phosphoramidates and phosphonamidates (ProTides) with antiviral activity. Antiviral Chemistry and Chemotherapy 26, pp. 1-31. (10.1177/2040206618775243)

2017

• Pertusati, F., Serafini, S., Albadry, N., Snoeck, R. and Andrei, G. 2017. Phosphonoamidate prodrugs of C5-substituted pyrimidine acyclic nucleosides for antiviral therapy. Antiviral Research 143, pp. 262-268. (10.1016/j.antiviral.2017.04.013)
• Serpi, M., De Biasi, R., Pertusati, F., Slusarczyk, M. and McGuigan, C. 2017. Synthetic approaches for the preparation of phosphoramidate prodrugs of 2’-deoxypseudoisocytidine. ChemistryOpen 6(3), pp. 424-436. (10.1002/open.201700019)
• Bassetto, M., Ferla, S., Giancotti, G., Pertusati, F., Westwell, A. D., Brancale, A. and McGuigan, C. 2017. Rational design and synthesis of novel phenylsulfonyl-benzamides as anti-prostate cancer agents. MedChemComm 8(7), pp. 1414-1420. (10.1039/C7MD00164A)
• James, E., Pertusati, F., Brancale, A. and McGuigan, C. 2017. Kinase-independent phosphoramidate S1P1 receptor agonist benzyl ether derivatives. Biorganic and Medicinal Chemistry Letters 27(6), pp. 1371-1378. (10.1016/j.bmcl.2017.02.011)
• Pertusati, F., Nutz, E., Kariuki, B. and Coogan, M. P. 2017. Synthesis and substrate-controlled reactions of 2,2′-unsaturated biquinazolinones. Tetrahedron 73(1), pp. 55-63. (10.1016/j.tet.2016.11.060)

2016

• Marinozzi, M., Pertusati, F. and Serpi, M. 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, M., Ferrari, V. and Pertusati, F. 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)
• Bassetto, M., Ferla, S., Pertusati, F., Kandil, S., Westwell, A., Brancale, A. and McGuigan, C. 2016. Design and synthesis of novel bicalutamide and enzalutamide derivatives as antiproliferative agents for the treatment of prostate cancer. European Journal of Medicinal Chemistry 118, pp. 230-243. (10.1016/j.ejmech.2016.04.052)
• Ferla, S., Bassetto, M., Pertusati, F., Kandil, S., Westwell, A. D., Brancale, A. and McGuigan, C. 2016. Rational design and synthesis of novel anti-prostate cancer agents bearing a 3,5-bis-trifluoromethylphenyl moiety. Bioorganic and Medicinal Chemistry Letters 26(15), pp. 3636-3640. (10.1016/j.bmcl.2016.06.001)
• McGuigan, C. et al. 2016. Anti-flavivirus activity of different tritylated pyrimidine and purine nucleoside analogues. ChemistryOpen 5(3), pp. 227-235. (10.1002/open.201500216)

2015

• Pertusati, F. and McGuigan, C. 2015. Diastereoselective synthesis of P-chirogenic phosphoramidate prodrugs of nucleoside analogues (ProTides) via copper catalysed reaction. Chemical Communications 51(38), pp. 8070-8073. (10.1039/C5CC00448A)
• Pertusati, F., McGuigan, C. and Serpi, M. 2015. Symmetrical diamidate prodrugs of nucleotide analogues for drug delivery. In: Current Protocols in Nucleic Acid Chemistry. Wiley-Blackwell, pp. 60:15.6.1-15.6.10., (10.1002/0471142700.nc1506s60)
• Ferrari, V., Serpi, M., McGuigan, C. and Pertusati, F. 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)

2014

• Toti, K. S. et al. 2014. Synthesis of an apionucleoside family and discovery of a prodrug with anti-HIV activity. Journal of Organic Chemistry 79(11), pp. 5097-5112. (10.1021/jo500659e)
• Pertusati, F., Hinsinger, K., Flynn, ?. S., Powell, N. G., Tristram, A. J., Balzarini, J. and McGuigan, C. 2014. PMPA and PMEA prodrugs for the treatment of HIV infections and human papillomavirus (HPV) associated neoplasia and cancer. European Journal of Medicinal Chemistry 78, pp. 259-268. (10.1016/j.ejmech.2014.03.051)
• McGuigan, C. et al. 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)

2013

• McGuigan, C. et al. 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)

2011

• Pertusati, F., Serpi, M. and McGuigan, C. 2011. Medicinal chemistry of nucleoside phosphonate prodrugs for antiviral therapy. Antiviral Chemistry and Chemotherapy 22(5), pp. 181-203. (10.3851/IMP2012)

2007

• Pertusati, F. 2007. Synthesis of atropisomeric 2,2'-disubstituted-3,3'-quinazolin-4,4'-diones and their application in asymmetric synthesis. PhD Thesis, Cardiff University.