Author: Kokosza, Kamil; Balzarini, Jan; Piotrowska, Dorota G.
Title: Design, synthesis, antiviral and cytostatic evaluation of novel isoxazolidine nucleotide analogues with a carbamoyl linker Cord-id: gxm0q0uw Document date: 2013_3_1
ID: gxm0q0uw
Snippet: 5-Arylcarbamoyl-2-methylisoxazolidin-3-yl-3-phosphonates have been synthesised from N-methyl-C-diethoxyphosphorylnitrone and N-arylacrylamides in good yields. cis- and trans-isoxazolidine phosphonates obtained herein were evaluated for activity against a broad range of DNA and RNA viruses. None of the compounds were endowed with antiviral activity at subtoxic concentrations. Isoxazolidines having phenyl substituted with halogen (Ar = 2-F-C(6)H(4); 3-Br-C(6)H(4); and 4-Br-C(6)H(4)) have been foun
Document: 5-Arylcarbamoyl-2-methylisoxazolidin-3-yl-3-phosphonates have been synthesised from N-methyl-C-diethoxyphosphorylnitrone and N-arylacrylamides in good yields. cis- and trans-isoxazolidine phosphonates obtained herein were evaluated for activity against a broad range of DNA and RNA viruses. None of the compounds were endowed with antiviral activity at subtoxic concentrations. Isoxazolidines having phenyl substituted with halogen (Ar = 2-F-C(6)H(4); 3-Br-C(6)H(4); and 4-Br-C(6)H(4)) have been found to inhibit proliferation of L1210, CEM as well as HeLa cells with IC(50) in the 100–170 μM range.
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