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Related Experiment Video

Updated: Apr 12, 2026

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Discovery and biological evaluation of 3-aryl-5-(3,4,5-trimethoxyphenyl)-5H-pyrrolo[2,3-b]pyrazine derivatives as

Wen Xu1, Yujing Zhang2, Qianqian Xu3

  • 1Department of Pharmacy, The Affiliated Hospital of Qingdao University, Qingdao, Shandong, 266003, China.

European Journal of Medicinal Chemistry
|April 10, 2026
PubMed
Summary

A novel compound, 10u, effectively inhibits tubulin polymerization and cancer cell growth. This promising anticancer agent shows significant tumor reduction in mice with minimal toxicity, supporting its therapeutic potential.

Keywords:
AnticancerMicrotubuleMolecular dockingTubulin inhibitorpyrrolo[2,3-b]pyrazine

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Area of Science:

  • Medicinal Chemistry
  • Molecular Biology
  • Oncology

Background:

  • Tubulin, the structural basis of microtubules, is a key target for anticancer drug development.
  • Small-molecule inhibitors of tubulin polymerization offer a promising strategy for novel cancer therapeutics.

Purpose of the Study:

  • To design, synthesize, and evaluate novel 3-aryl-5-(3,4,5-trimethoxyphenyl)-5H-pyrrolo[2,3-b]pyrazine derivatives as tubulin polymerization inhibitors.
  • To identify potent anticancer agents with potential therapeutic applications.

Main Methods:

  • Rational drug design based on structural analysis of known tubulin inhibitors and computational models.
  • Synthesis of a focused library of pyrrolo[2,3-b]pyrazine derivatives.
  • In vitro antiproliferative activity assays against human cancer cell lines (Huh7, HeLa, A549).
  • Mechanistic studies including tubulin polymerization assays, cell cycle analysis, and apoptosis induction.
  • In vivo efficacy and toxicity assessment in an orthotopic Huh7 mouse model.

Main Results:

  • Compound 10u exhibited potent antiproliferative activity with IC50 values in the nanomolar range (0.085-0.13 μM) against tested cancer cell lines.
  • 10u effectively inhibited tubulin polymerization, disrupted the microtubule network, induced G2/M cell cycle arrest, and triggered apoptosis.
  • In vivo studies demonstrated significant tumor growth inhibition in an orthotopic mouse model with no observable systemic toxicity.

Conclusions:

  • Compound 10u is a potent inhibitor of tubulin polymerization with significant anticancer activity.
  • 10u demonstrates promising dual-phase anticancer effects and warrants further development as a potential therapeutic agent.