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A novel and efficient one-pot synthesis of symmetrical diamide (bis-amidate) prodrugs of acyclic nucleoside phosphonates and evaluation of their biological activities.
Jansa P, Baszczyňski O, Dračínský M, Votruba I, Zídek Z, Bahador G, Stepan G, Cihlar T, Mackman R, Holý A, Janeba Z. Jansa P, et al. Among authors: cihlar t. Eur J Med Chem. 2011 Sep;46(9):3748-54. doi: 10.1016/j.ejmech.2011.05.040. Epub 2011 May 23. Eur J Med Chem. 2011. PMID: 21664011
No virologic resistance to bulevirtide monotherapy detected in patients through 24 weeks treatment in phase II and III clinical trials for chronic hepatitis delta.
Hollnberger J, Liu Y, Xu S, Chang S, Martin R, Manhas S, Aeschbacher T, Han B, Yazdi T, May L, Han D, Shornikov A, Flaherty J, Manuilov D, Suri V, Asselah T, Lampertico P, Wedemeyer H, Aleman S, Richards C, Mateo R, Maiorova E, Cihlar T, Mo H, Urban S. Hollnberger J, et al. Among authors: cihlar t. J Hepatol. 2023 Sep;79(3):657-665. doi: 10.1016/j.jhep.2023.04.027. Epub 2023 Apr 27. J Hepatol. 2023. PMID: 37120031 Clinical Trial.
Synthesis, anti-HIV activity, and resistance profile of thymidine phosphonomethoxy nucleosides and their bis-isopropyloxymethylcarbonyl (bisPOC) prodrugs.
Mackman RL, Zhang L, Prasad V, Boojamra CG, Douglas J, Grant D, Hui H, Kim CU, Laflamme G, Parrish J, Stoycheva AD, Swaminathan S, Wang K, Cihlar T. Mackman RL, et al. Among authors: cihlar t. Bioorg Med Chem. 2007 Aug 15;15(16):5519-28. doi: 10.1016/j.bmc.2007.05.047. Epub 2007 May 25. Bioorg Med Chem. 2007. PMID: 17562366
Design and profiling of GS-9148, a novel nucleotide analog active against nucleoside-resistant variants of human immunodeficiency virus type 1, and its orally bioavailable phosphonoamidate prodrug, GS-9131.
Cihlar T, Ray AS, Boojamra CG, Zhang L, Hui H, Laflamme G, Vela JE, Grant D, Chen J, Myrick F, White KL, Gao Y, Lin KY, Douglas JL, Parkin NT, Carey A, Pakdaman R, Mackman RL. Cihlar T, et al. Antimicrob Agents Chemother. 2008 Feb;52(2):655-65. doi: 10.1128/AAC.01215-07. Epub 2007 Dec 3. Antimicrob Agents Chemother. 2008. PMID: 18056282 Free PMC article.
Stray, K.-Y. Lin, Y. Gao, R. L. Mackman, and T. Cihlar, Antimicrob. Agents Chemother. 52:648-654, 2008). GS-9148 diphosphate acts as a competitive inhibitor of RT with respect to dATP (K(i) = 0.8 muM) and exhibits low inhibitory potency against host polymerases incl …
Stray, K.-Y. Lin, Y. Gao, R. L. Mackman, and T. Cihlar, Antimicrob. Agents Chemother. 52:648-654, 2008). GS-9148 diphosphate a …
Synthesis and anti-HIV activity of cyclic pyrimidine phosphonomethoxy nucleosides and their prodrugs: a comparison of phosphonates and corresponding nucleosides.
Mackman RL, Zhang L, Prasad V, Boojamra CG, Chen J, Douglas J, Grant D, Laflamme G, Hui H, Kim CU, Parrish J, Stoycheva AD, Swaminathan S, Wang K, Cihlar T. Mackman RL, et al. Among authors: cihlar t. Nucleosides Nucleotides Nucleic Acids. 2007;26(6-7):573-7. doi: 10.1080/15257770701490126. Nucleosides Nucleotides Nucleic Acids. 2007. PMID: 18066858
154 results