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

Ubaldina Galli, Cristina Travelli, Silvio Aprile, Elena Arrigoni, Simone Torretta, Giorgio Grosa, Alberto Massarotti, Giovanni Sorba, Pier Luigi Canonico, Armando A. Genazzani, Gian Cesare Tron

Research output: Contribution to journalArticlepeer-review

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.

Original languageEnglish
Pages (from-to)1345-1357
Number of pages13
JournalJournal of Medicinal Chemistry
Volume58
Issue number3
DOIs
Publication statusPublished - 12 Feb 2015

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