Vascular disrupting activity of tubulin-binding 1,5-diaryl-1H-imidazoles

Katiuscia Bonezzi, Giulia Taraboletti, Patrizia Borsotti, Fabio Bellina, Renzo Rossi, Raffaella Giavazzi

Research output: Contribution to journalArticle

Abstract

Highly cytotoxic 1,5-diaryl-1H-imidazoles were studied to clarify the relationship between cytotoxicity and activity as vascular disrupting agents (VDA). All the compounds disorganized the tubulin cytoskeleton, affected endothelial cell morphology and capillary formation in vitro, and caused vessel shutdown and tumor necrosis in vivo, thus confirming their vascular disrupting properties. Nonetheless, the substitution patterns on the imidazole ring, responsible for greater interaction energy with tubulin and higher cytotoxicity, were not associated to greater vascular disrupting activity.

Original languageEnglish
Pages (from-to)7906-7910
Number of pages5
JournalJournal of Medicinal Chemistry
Volume52
Issue number23
DOIs
Publication statusPublished - Dec 10 2009

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ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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