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July 23, 2026Journal of Medicinal Chemistry

Structural Modification and Prodrug Design Based on Natural Stilbene Scaffold for the Discovery of Novel PARP-1 Inhibitors with Improved Antitumor Activity

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Authors

ZZZhiru ZouGLGuoqing LuMXMeixiu Xin

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Overview

Randomized trial discovers potent antitumor agents in BRCA-deficient models, indicating new therapeutic avenues.

Key Points

  • The study aims to discover novel PARP-1 inhibitors using structural modifications of a natural stilbene scaffold.
  • Designed and synthesized stilbene derivatives with an ortho-hydroxybenzamide scaffold.
  • Evaluated the antiproliferative activity against BRCA1 and BRCA2-deficient cell lines.
  • Developed ROS-responsive prodrugs to enhance in vivo efficacy.
  • Compound 24c exhibited potent antiproliferative activity against BRCA1-deficient cell lines with significant effects on cell cycle and apoptosis.
  • P-24c demonstrated excellent antitumor activity with a tumor growth inhibition of 69.3% in a SUM149PT xenograft model.
  • The developed inhibitors effectively inhibited PARP-1 activity and induced oxidative stress, leading to cell death.

Cite This Study

Zou et al. (2026) studied this question.

synapsesocial.com/papers/6a61aea0faa9903c51169d43https://doi.org/10.1021/acs.jmedchem.6c01564
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