Design, synthesis, and biological evaluation of combretabenzodiazepines: A novel class of anti-tubulin agents
Articolo
Data di Pubblicazione:
2015
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.
Tipologia CRIS:
1.1 Articolo in rivista
Keywords:
Antineoplastic Agents; Benzodiazepinones; Cell Proliferation; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Molecular Structure; Structure-Activity Relationship; Tubulin; Tubulin Modulators; Tumor Cells, Cultured; Drug Design
Elenco autori:
Galli, U.; Travelli, C.; Aprile, S.; Arrigoni, E.; Torretta, S.; Grosa, G.; Massarotti, A.; Sorba, G.; Canonico, P. L.; Genazzani, A. A.; Tron, G. C.
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