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  2. Deploying solid-phase synthesis to access thymine-containing nucleoside analogs that inhibit DNA repair nuclease SNM1A

Deploying solid-phase synthesis to access thymine-containing nucleoside analogs that inhibit DNA repair nuclease SNM1A

  • Org Biomol Chem. 2023 Jul 19;21(28):5873-5879. doi: 10.1039/d3ob00836c.
Christine A Arbour 1 Ellen M Fay 2 Joanna F McGouran 2 Barbara Imperiali 1
Affiliations

Affiliations

  • 1 Department of Biology and Department of Chemistry, Massachusetts Institute of Technology, Cambridge, MA 02139, USA. imper@mit.edu.
  • 2 School of Chemistry and Trinity Biomedical Sciences Institute, Trinity College Dublin, 152-160 Pearse St., Dublin 2, Ireland.
Abstract

Nucleoside analogs show useful bioactive properties. A versatile solid-phase synthesis that readily enables the diversification of thymine-containing nucleoside analogs is presented. The utility of the approach is demonstrated with the preparation of a library of compounds for analysis with SNM1A, a DNA damage repair Enzyme that contributes to cytotoxicity. This exploration provided the most promising nucleoside-derived inhibitor of SNM1A to date with an IC50 of 12.3 μM.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-155595
    SNM1A抑制剂