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a values of 2, 4-dioxobutanoic acids (ca. 2.1 and 7.6, in water), and complexation studies, are clearly in favour; see
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a values of 2, 4-dioxobutanoic acids (ca. 2.1 and 7.6, in water), and complexation studies, are clearly in favour; see: T.Z. Verbic, B.J. Drakulic, M.F. Zloh, J.R. Pecelj, G.V. Popovic, and I.O. Juranic J. Serb. Chem. Soc. 72 2007 1201 1216
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also see: A. Bacchi, M. Carcelli, C. Compari, E. Fisicaro, N. Pala, G. Rispoli, D. Rogolino, T.W. Sanchez, M. Sechi, and N. Neamati Mol. Pharmaceutics 8 2011 507 519
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The working hypothesis of the senior author was and is that even the truncated viral oligodeoxynucleotides incorporating INI-like fragments could render inactive the pre-integration complex and/or may contribute to the blocking of IN in vivo. On the other hand, a simple mixing of L-708,906 (INI) with AZT (NRTI) was proved to be sub-synergistic:, (addition of the INI could be postponed for 7 h after infection)
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The working hypothesis of the senior author was and is that even the truncated viral oligodeoxynucleotides incorporating INI-like fragments could render inactive the pre-integration complex and/or may contribute to the blocking of IN in vivo. On the other hand, a simple mixing of L-708,906 (INI) with AZT (NRTI) was proved to be sub-synergistic: W. Pluymers, G. Pais, B. Van Maele, C. Pannecouque, V. Fikkert, T.R. Burke, E. De Clercq, M. Witvrouw, N. Neamati, and Z. Debyser Antimicrob. Agents Chemother. 46 2002 3292 3297 (addition of the INI could be postponed for 7 h after infection)
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41149151814
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Evaluated with the MTT method [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide] in MT-4 cells. Stock solutions of the compounds were prepared in DMSO (10 mg/mL). After 4 days of incubation at 37 °C, the number of viable cells was determined with MTT. Standard parallel tests for cytotoxic effects in uninfected MT-4 cells were always performed. See, e.g.
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Evaluated with the MTT method [3-(4, 5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide] in MT-4 cells. Stock solutions of the compounds were prepared in DMSO (10 mg/mL). After 4 days of incubation at 37 °C, the number of viable cells was determined with MTT. Standard parallel tests for cytotoxic effects in uninfected MT-4 cells were always performed. See, e.g.: G. Moncunill, M. Armand-Ugon, I. Clotet-Codina, E. Pauls, E. Ballana, A. Llano, B. Romagnoli, J.W. Vrijbloed, F.O. Gombert, B. Clotet, S. De Marco, and J.A. Este Mol. Pharmacol. 73 2008 1264
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Many thymidine analogues are substrates for thymidine kinase 2 (mitochondrial TK2), for the monophosphorylation rate-limiting step. For a review, see
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Many thymidine analogues are substrates for thymidine kinase 2 (mitochondrial TK2), for the monophosphorylation rate-limiting step. For a review, see: M.-J. Pérez-Pérez, E.-M. Priego, A.-I. Hernández, O. Familiar, M.-J. Camarasa, A. Negri, F. Gago, and J. Balzarini Med. Res. Rev. 28 2008 797 820
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nonpolar nucleoside mimics are phosphorylated by TK2 (but not by TK1)
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nonpolar nucleoside mimics are phosphorylated by TK2 (but not by TK1) S.K. Jarchow-Choy, E. Sjuvarsson, H.O. Sintim, S. Eriksson, and E.T. Kool J. Am. Chem. Soc. 131 2009 5488 5494
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For the advantages of acyl cyanides (2-oxonitriles) in the C-acylation of enolates (in general), avoiding the formation of O-acylated by-products, see
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For the advantages of acyl cyanides (2-oxonitriles) in the C-acylation of enolates (in general), avoiding the formation of O-acylated by-products, see: C. Wiles, P. Watts, S.J. Haswell, and E. Pombo-Villar Tetrahedron Lett. 43 2002 2945 2948
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1642495629
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2, pH 7.0, 37 °C, according to
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2, pH 7.0, 37 °C, according to: E. Deprez, S. Barbe, M. Kolaski, H. Leh, F. Zouhiri, C. Auclair, J.C. Brochon, M. Le Bret, and J.F. Mouscadet Mol. Pharmacol. 65 2004 85 98
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Mouscadet, J.F.9
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30
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62149093020
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50 values were determined 48 h post infection as the concentration of drug inhibiting β-galactosidase production by 50% in comparison to results for the untreated infected cells. Cytotoxicities were determined in parallel on uninfected cells
-
50 values were determined 48 h post infection as the concentration of drug inhibiting β-galactosidase production by 50% in comparison to results for the untreated infected cells. Cytotoxicities were determined in parallel on uninfected cells
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Subra, F.7
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Mouscadet, J.F.9
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