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June 10, 2026RSC Medicinal Chemistry

Targeting DNA-PK: medicinal chemistry insights into small-molecule inhibitor discovery and optimisation

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Authors

EWElle WatsonJHJack R. R. HutchinsonSHSuzannah J. Harnor

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Overview

Review highlights the discovery and optimization of DNA-PK inhibitors, indicating their potential in treatment.

Key Points

  • This review aims to provide insights into the discovery and optimization of DNA-PK inhibitors for therapeutic use.
  • Reviewed the synthesis of DNA-PK inhibitors from early hits to clinical candidates.
  • Discussed the pharmacological profiles of optimized scaffolds like chromen-4-ones and purinones.
  • Highlighted the advancements in DNA-PK inhibitor development since Wortmannin.
  • Provided examples of optimized inhibitors such as NU5455 and AZD7648.

Cite This Study

Watson et al. (2026) studied this question.

synapsesocial.com/papers/6a28fecb6f82f25be989c068https://doi.org/10.1039/d6md00119j
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