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Page 1
Phosphoramidate ProTides of 2'-C-methylguanosine as highly potent inhibitors of hepatitis C virus. Study of their in vitro and in vivo properties.
McGuigan C, Gilles A, Madela K, Aljarah M, Holl S, Jones S, Vernachio J, Hutchins J, Ames B, Bryant KD, Gorovits E, Ganguly B, Hunley D, Hall A, Kolykhalov A, Liu Y, Muhammad J, Raja N, Walters R, Wang J, Chamberlain S, Henson G. McGuigan C, et al. Among authors: madela k. J Med Chem. 2010 Jul 8;53(13):4949-57. doi: 10.1021/jm1003792. J Med Chem. 2010. PMID: 20527890
Design, synthesis and evaluation of a novel double pro-drug: INX-08189. A new clinical candidate for hepatitis C virus.
McGuigan C, Madela K, Aljarah M, Gilles A, Brancale A, Zonta N, Chamberlain S, Vernachio J, Hutchins J, Hall A, Ames B, Gorovits E, Ganguly B, Kolykhalov A, Wang J, Muhammad J, Patti JM, Henson G. McGuigan C, et al. Among authors: madela k. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4850-4. doi: 10.1016/j.bmcl.2010.06.094. Epub 2010 Jun 20. Bioorg Med Chem Lett. 2010. PMID: 20637609
Phosphorodiamidates as a promising new phosphate prodrug motif for antiviral drug discovery: application to anti-HCV agents.
McGuigan C, Madela K, Aljarah M, Bourdin C, Arrica M, Barrett E, Jones S, Kolykhalov A, Bleiman B, Bryant KD, Ganguly B, Gorovits E, Henson G, Hunley D, Hutchins J, Muhammad J, Obikhod A, Patti J, Walters CR, Wang J, Vernachio J, Ramamurty CV, Battina SK, Chamberlain S. McGuigan C, et al. Among authors: madela k. J Med Chem. 2011 Dec 22;54(24):8632-45. doi: 10.1021/jm2011673. Epub 2011 Nov 16. J Med Chem. 2011. PMID: 22039920
Design, synthesis and biological evaluation of phosphorodiamidate prodrugs of antiviral and anticancer nucleosides.
McGuigan C, Bourdin C, Derudas M, Hamon N, Hinsinger K, Kandil S, Madela K, Meneghesso S, Pertusati F, Serpi M, Slusarczyk M, Chamberlain S, Kolykhalov A, Vernachio J, Vanpouille C, Introini A, Margolis L, Balzarini J. McGuigan C, et al. Among authors: madela k. Eur J Med Chem. 2013;70:326-40. doi: 10.1016/j.ejmech.2013.09.047. Epub 2013 Oct 9. Eur J Med Chem. 2013. PMID: 24177359 Free PMC article.
INX-08189, a phosphoramidate prodrug of 6-O-methyl-2'-C-methyl guanosine, is a potent inhibitor of hepatitis C virus replication with excellent pharmacokinetic and pharmacodynamic properties.
Vernachio JH, Bleiman B, Bryant KD, Chamberlain S, Hunley D, Hutchins J, Ames B, Gorovits E, Ganguly B, Hall A, Kolykhalov A, Liu Y, Muhammad J, Raja N, Walters CR, Wang J, Williams K, Patti JM, Henson G, Madela K, Aljarah M, Gilles A, McGuigan C. Vernachio JH, et al. Among authors: madela k. Antimicrob Agents Chemother. 2011 May;55(5):1843-51. doi: 10.1128/AAC.01335-10. Epub 2011 Feb 28. Antimicrob Agents Chemother. 2011. PMID: 21357300 Free PMC article.
Synthesis of phosphoramidate prodrugs: ProTide approach.
Serpi M, Madela K, Pertusati F, Slusarczyk M. Serpi M, et al. Among authors: madela k. Curr Protoc Nucleic Acid Chem. 2013 Jun;Chapter 15:15.5.1-15.5.15. doi: 10.1002/0471142700.nc1505s53. Curr Protoc Nucleic Acid Chem. 2013. PMID: 23775807
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