Prof Chris McGuigan - BSc PhD
Link to a complete list of Prof McGuigan's publications since 2001
2010:
Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepititis C virus. C. McGuigan, K. Madela, M. Aljarah, A. Gilles, A. Brancale, N. Zonte, S. Chamberlain, J. Vernachio, J. Hutchins, A. Hall, B. Ames, E. Gorovits, B Ganguly, A. Kolykhalov, J. Wang, J. Muhamad, J. M. Patti, G. Henson. BMCL, 2010, 4850-4854.
Design, synthesis and biological evaluation of novel phosphoramidate ProTides of the 2’-fluoro derivative of potent anti-VZV BCNA. M. Derudas, M. Quintiliani, A. Brancale, G. Andrei, R. Snoeck, J. Balzarini, C. McGuigan. AVCC, 2010. In press.
Phosphoramidate ProTides of 2’-C-Methylguanosine as highly potent inhibitors of hepatitis C virus. Study of their in vitro and in vivo properties. C. McGuigan, A. Gilles, K. Madela, M. Aljarah, S. Holl, S. Jones, J. Vernachio, J. Hutchins, B. Ames, D. Bryant, E. Gorovits, B. Ganguly, D. Hunley, A. Hall, A. Kolykhalov, Y, Liu, J. Muhammad, N. Raja, R. Walters, J. Wang, S. Chamberlain, G. Henson. J. Med. Chem., 2010, 4949-4957.
Penylboronic acid-based carbohydrate binders as antiviral therapeutics I: Mono-phenylboronic acids. P. Trippier, C. McGuigan, J. Balzarini. AVCC-10-OA-0020.R1, 2010. In Press
The Design, Synthesis and Antiviral Evaluation of a Series of 5-Trimethylsilyl-1-β-D(Arabinofuranosyl)uracil Phosphoramidate ProTides. Y. Mehellou, J. Balzarini, C. McGuigan. AVCC, 2010, 20(4):153-60.
A New Class of Dual-Targeted Antivirals: Monophosphorylated Acyclovir Prodrug Derivatives Suppress Both Human Imunodeficiency Virus Type 1 and Herpes Simplex Virus Type 2. C. Vanpouille, A. Lisco, M. Derudas, E. Saba, J-C Grivel, B. Brichacek, F. Scrimieri, R. Schinazi, D. Schols, C. McGuigan, J. Balzarini, L. Margolis. J. Infect. Dis., 2010, 201, 4, 635-643.
Application of the Phosphoramidate ProTide Approach to the Antiviral Drug Ribavirin. M. Derudas, A. Brancale, L. Naesens, J. Neyts, J. Balzarini, C. McGuigan. BMC, 18, 2010, 2748-2755.
Phosphoramidates of 2’-B-D-arabinouridine (AraU) as phosphate prodrugs; Design, synthesis, in vitro activity and metabolism. Y Mehellou, R. Valente, H. Mottram, E. Walsby, K I Mills, J. Balzarini, C. McGuigan. BMC, 18, 2010, 2439-2446.
2009:
Mechanisms Associated with HIV-1 Resistance to Acyclovir by the V75I Mutation in Reverse Transcriptase. E. P. Tchesnokov, A. Obikhod, I. Massud, A. Lisco, C. Vanpouille, B. Brichacek, J. Balzarini, C. McGuigan, M. Derudas, L. Margolis, R. F. Schinazi, M. Gotte. Journal of Biological Chemistry, 2009, 284, 32, 21496-21504.
FV100 as a new approach for the possible treatment of Varicella Zoster Virus. C. McGuigan, J. Balzarini. Antimicrobial Chemotherapy, 2009, 64, 671-673.
Aryloxy Phosphoramidate Triesters: A Technology for delivering mono-phosphorylated nucleosides and sugars into cells. C. McGuigan, Y. Mehellou, J. Balzarini, ChemMedChem, 2009, 4, 11, 1779-1791.
2’-Fluorosugar analogues of the highly potent anti-varicella-zoster virus-bicyclic nucleoside analogue (BCNA) Cf 1743. C McGuigan, M Derudas, M Quintiliani, G. Andrei, R. Snoeck, G Henson, J Balzarini. BMCL, 2009, 19, 6264-6267.
The Application of Phosphoramidate ProTide Technology to the Potent Anti-HCV Compound 4′-Azidocytidine. C. McGuigan, M.R. Kelleher, P. Perrone, S. Mulready, G. Luoni, F. Daverio, K. Klumpp and D.B. Smith. BMCL, 19, 2009, 4250-4254.
The phosphoramidate approach greatly enhances the biological activity of β-2’methyl-purines against Hepititis C Virus. C. McGuigan, P. Perrone, K. Madela, Johan Neyts. BMCL, 19, 2009, 4316-4320.
Alkenyl Substituted Bicyclic Nucleoside Analogues Retain Nanomolar potency against Varicella Zoster Virus” C. McGuigan, O. Bidet, M. Derudas, G. Andrei, R. Snoeck, J. Balzarini. BMC, 2009, 17, 3025-7.
The Application of the Phosphoramidate ProTide Approach confers micromolar Potency against Hepatitis C Virus on Inactive Agent 4’- Azidoinosine: Kinase Bypass on a Dual Base/Sugar Modified Nucleoside” C. McGuigan, F. Daverio, I. Najera, J.A. Martin, K. Klumpp, D. Smith. BMCL, 2009, 19, 3122-4
In Vitro Activity and In Vivo Pharmockinetics of Highly Potent Phosphoramidate Nucleoside Analogue Inhibitors of Hepatitis C NSSB. J. Hutchins, S Chamberlain, C Chang, B Ganguly, E Gorovits, A Hall, G Henson, A Kolykhalov, Y Liu, J Muhammad, P Perrone, A Gilles S Holl, K Madela, C McGuigan, J Patti. 22nd International Conference on Antiviral Research, 2009, Miami, ANTIVIRAL RESEARCH, VL 82, A1-A83.
Phosphoramidate Protides Greatly Enhance the Anti-HCV Activity of 2′ - Methylguanosine. K Madela P Perrone, A. Gilles, J. Neyts, C. McGuigan. 22nd International Conference on Antiviral Research, 2009, Miami, ANTIVIRAL RESEARCH, VL , A1-A83.
Synthesis and Evaluation of Novel Acyclovir Phosphoramidates as Anti-HIV Agents. D. Carta, C. McGuigan, L. Margolis, J. Balzarini. 22nd International Conference on Antiviral Research, 2009, Miami, ANTIVIRAL RESEARCH, VL , A1-A83.
The Application of Phosphoramidate Protide Technology to Acyclovir Confers Novel Anti-HIV Inhibition. M. Derudas, C. McGuigan, A. Brancale, L. Margolis, J. Balzarini. 22nd International Conference on Antiviral Research, 2009, Miami, ANTIVIRAL RESEARCH, VL , A1-A83.
Design, Synthesis, and Biological Evaluation of Novel Fluoro Derivatives of BCNA. M. Derudas, M. Quintiliani, C. McGuigan, A. Brancale , G. Henson , J. Balzarini. 22nd International Conference on Antiviral Research, 2009, Miami, ANTIVIRAL RESEARCH, VL 82, A1-A83
2008:
“Molecular modelling studies on the Binding of some protides to a putative human phosphoramidase Hint1”, C. Congiatu, A. Brancale, C. McGuigan. Nucleosides, Nucleotides and Nucleic Acids, 26: 2008, 1121-1124.
“Successful kinase bypass with new acyclovir phosphoramidate prodrugs”. C. McGuigan, M. Derudas, J. Bugert, G. Andrei, R. Snoeck, J. Balzarini. BioOrg Med Chem Lett., 2008, 4364-4367.
“Acyclovir Is Activated into a HIV-1 Reverse Transcriptase Inhibitor in Herpesvirus-Infected Human Tissues” A. Lisco, C.
Vanpouille, E. P. Tchesnokov, J-C Grivel, A. Biancotto, B. Brichacek, J. Elliott, E. Fromentin, R. Shattock, P. Anton, R. Gorelick, J. Balzarini, C. McGuigan, M. Derudas, M. Götte, R. F. Schinazi, L. Margolis. Cell Host & Microbe, Volume 4, Issue 3, 2008, 260-270
“Phosphate Prodrugs Derived From N-Acetylglucosamine Have Enhanced Chondroprotective Activity in Explant Cultures and Represent a New Lead in Anti-Osteoarthritis Drug Discovery". C. McGuigan, M. Serpi, R. Bibbo, H. Roberts, C. Hughes, B. Caterson, A. Gibert, C. Verson. J. Med. Chem., 2008, 51, 5807-5812.
“Activation of p16 gene silenced by DNA ethylation in cancer cells by phosphoramidate derivatives of 2’-deoxyzebularine” C. McGuigan, V Marquez, C Yoo, R. Valente, C. Congiatu, F. Gavazza, A. Angel, A. Siddiqui, P. Jones. J., Med. Chem., 2008, 51, 7593-7601
“Design, synthesis and evaluation of novel Anti-VZV BCNAs”, C. McGuigan, M. Migliore, G. Henson, J. Patti, G. Andrei, R. Snoeck, J. Balzarini. 21st International Conference on Antiviral Research. 2008, CL Montreal, ANTIVIRAL RESEARCH, VL 78, A1-A76, 33.
“Design and synthesis of novel non-nucleoside anti-HCMV agents”. R. Adak, C. McGuigan, R. Snoeck, G. Andrei, J. Balzarini, E. Gorovits, C. Chang, B. Ames, Y. Liu, J. Vernachio. 21st International Conference on Antiviral Research, 2008, CL Montreal, ANTIVIRAL RESEARCH, VL 78, IS 2, A1-A76, 93.
“Design, synthesis and biological evaluation of novel acyclovir ProTides”. M. Derudas, C. McGuigan, A. Brancale, J. Bugert, G. Andrei, R. Snoeck, J. Balzarini, J., CT 21st International Conference on Antiviral Research, CY, 2008, CL Montreal, ANTIVIRAL RESEARCH, VL 78, IS 2, BP A1-A76, 102.
“Application of the Phosphoramidate Protide Approach to the Antiviral Drug Ribavirin” M. Derudas, C. McGuigan, A. Brancale, J. Neyts, J. Balzarini. CT 21st International Conference on Antiviral Research, CY, 2008, CL Montreal, ANTIVIRAL RESEARCH, VL 78, IS 2, BP A1-A76, 101.
2007:
Perrone, P., Luoni, G.M., Kelleher, M-R., Daverio, F., Angell, A., Mulready, S., Congiatu, C., Rajyaguru, S., Martin, J.A., Lévêue, V., Le Pogam, S. Najera, I.I., Klumpp, K., Smith, D.B., McGuigan. C. Application of the Phosphoramidate ProTide Approach to 4’-Azidouridine Confers sub-µM Potency versus Hepatitis C Virus on an inactive Nucleoside. J. Med Chem, 2007, 50, 1840-1849.
Mehellou, Y., McGuigan, C., Brancale, A., Balzarini. J. Design, synthesis, and anti-HIV activity of 20,30-didehydro-20,30-dideoxyuridine (d4U), 20,30-dideoxyuridine (ddU) phosphoramidate ‘ProTide’ derivatives. Bioorganic & Medicinal Chemistry Letters 17 (2007) 3666–3669.
Perrone, P., Daverio, F., Valente, R., Rajyaguru, S., Martin, J., Leveque, V., LePogam, S., Najera, I., Klumpp, K., Smith, D., McGuigan. C. First example of Phosphomaidate Approach Applied to a 4’-Substituted Purine Nucleoside (4’-Azidoadenosine): Conversion of an Inactive Nucleoside to a Submicromolar Compound versus Hepatitis C Virus. J. Med Chem., 2007, 50, 5463-5470.
McGuigan, C., Pathirana, R.N., Migliore, M., Adak, R., Luoni, G., Jones, A.T., Diez-Torrubia, A., Camarasa, M-J., Velazquez, S., Henson, G., Verbeken, E., Sienaert, R., Naesens, L., Snoeck, R, Andrei, G., Balzarini, J. Preclinical development of bicyclic nucleoside analogues as potent and selective inhibitors of varicella zoster virus. Journal of Antimicrobial Chemotherapy, 2007, 60, 1316-1330.
Migliore, M., Zonta, N., McGuigan, C., Henson, G., Andrei, G., Snoeck, R., Balzarini. J. Synthesis and Antiviral Activity of the Carbocyclic Analogue of the Highly Potent and Selective Anti-VZV Bicyclo Furano Pyrimidines (BCNAs). J. Med. Chem, 2007, 50, 6485-6492.
Derudas, M., McGuigan, C., Snoeck, R., Andrei, G., De Clercq, E., Balzarini. J. Design, Synthesis and Biological Evaluaiton of Novel AntiVZV Agents. Program and Abstracts/Antiviral Research 74 (2007), 108, A72.
Adak, R., McGuigan, C., Snoeck, R., Andrei, G., De Clercq, E., Balzarini. J. Design and Synthesis of Novel anti-HCMV Agents: Modifications to the Bicyclic Pyrimidine Base. Program and Abstracts/Antiviral Research 74 (2007), 106, A71.
Congiatu, C., McGuigan, C., Brancale A. HINT as Putative Phosphoramidase Responsible of Pro-Tides Activation: Molecular Modelling Studies. Program and Abstracts/Antiviral Research 74 (2007), 107, A71.
Mehellou, Y., McGuigan, C., Balzarini. J. The Design, Synthesis and Anti-HIV Activity of a Selected Group of 2’,3’-Didehydro-2’,3’-Dideoxyguanosine (d4G) and 2’,3’-Dideoxyguanosine (ddG) ‘PtoTide’ Derivatives. Program and Abstracts/Antiviral Research 74 (2007), 55, A50.