2. Academic Validation
  3. Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents

Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents

  • J Med Chem. 2015 Feb 12;58(3):1345-57. doi: 10.1021/jm5016389.
Ubaldina Galli 1,  Cristina Travelli,  Silvio Aprile,  Elena Arrigoni,  Simone Torretta,  Giorgio Grosa,  Alberto Massarotti,  Giovanni Sorba,  Pier Luigi Canonico,  Armando A Genazzani,  Gian Cesare Tron
Affiliations

Affiliation

  • 1 Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale "A. Avogadro" , Largo Donegani 2, 28100 Novara, Italy.
PMID: 25584687 DOI: 10.1021/jm5016389
Abstract

In the present manuscript, starting from the 1,4-benzodiazepin-2-one nucleus, a privileged structure in medicinal chemistry, we have synthesized a novel class of cis-locked combretastatins named combreatabenzodiazepines. They show similar cytotoxic and antitubulin activity compared to combretastatin A-4 in neuroblastoma cells, showing a better pharmacokinetic profile. This class of compounds has therefore the potential for further development as antitubulin agents.

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