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

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.

DOI: 10.1021/jm5016389

Cite this paper

@article{Galli2015DesignSA, title={Design, synthesis, and biological evaluation of combretabenzodiazepines: a novel class of anti-tubulin agents.}, author={Ubaldina Galli and Cristina Travelli and Silvio Aprile and Elena Arrigoni and Simone Torretta and Giorgio Grosa and Alberto Massarotti and Giovanni Sorba and Pier Luigi Canonico and Armando A Genazzani and Gian Cesare Tron}, journal={Journal of medicinal chemistry}, year={2015}, volume={58 3}, pages={1345-57} }