Issue 28, 2023

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

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.

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

Supplementary files

Article information

Article type
Paper
Submitted
26 May 2023
Accepted
25 Jun 2023
First published
26 Jun 2023

Org. Biomol. Chem., 2023,21, 5873-5879

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

C. A. Arbour, E. M. Fay, J. F. McGouran and B. Imperiali, Org. Biomol. Chem., 2023, 21, 5873 DOI: 10.1039/D3OB00836C

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