Selected article for: "activity relationship and Structure activity relationship"

Author: Qi Liu; Amita Gupta; Ayse Okesli-Armlovich; Wenjie Qiao; Curt R. Fischer; Mark Smith; Jan E. Carette; Michael C. Bassik; Chaitan Khosla
Title: Enhancing the Antiviral Efficacy of RNA-Dependent RNA Polymerase Inhibition by Combination with Modulators of Pyrimidine Metabolism
  • Document date: 2020_3_25
  • ID: 1zk64gsg_8
    Snippet: Due to the high toxicity of CPC, we undertook structure-activity relationship (SAR) analysis of CPU wherein uracil nucleobase was maintained intact or only modified at the C5 position. Meanwhile, the C-5' substituent of CPU was modified, because this is the site of UCK2-catalyzed phosphorylation. In order to rapidly access both nucleobase and carbocyclic moiety analogs, we implemented a diversity-oriented synthetic approach featuring a Mitsunobu .....
    Document: Due to the high toxicity of CPC, we undertook structure-activity relationship (SAR) analysis of CPU wherein uracil nucleobase was maintained intact or only modified at the C5 position. Meanwhile, the C-5' substituent of CPU was modified, because this is the site of UCK2-catalyzed phosphorylation. In order to rapidly access both nucleobase and carbocyclic moiety analogs, we implemented a diversity-oriented synthetic approach featuring a Mitsunobu reaction as the strategic transformation (Choi et al., 2012) .

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