N-Hydroxyimides and hydroxypyrimidinones as inhibitors of the DNA repair complex ERCC1–XPF
2015
Abstract A high throughput screen allowed the identification of N -hydroxyimide inhibitors of ERCC1–XPF endonuclease activity with micromolar potency, but they showed undesirable selectivity profiles against FEN-1. A scaffold hop to a hydroxypyrimidinone template gave compounds with similar potency but allowed selectivity to be switched in favour of ERCC1–XPF over FEN-1. Further exploration of the structure–activity relationships around this chemotype gave sub-micromolar inhibitors with >10-fold selectivity for ERCC1–XPF over FEN-1.
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