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.

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

GALLI, Ubaldina;GROSA, Giorgio;SORBA, Giovanni;CANONICO, Pier Luigi;GENAZZANI, Armando
;
TRON, Gian Cesare
2015-01-01

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.
2015
58
3
1345
1357
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
GALLI, Ubaldina; TRAVELLI, Cristina; APRILE, SILVIO; Arrigoni, Elena; TORRETTA, SIMONE; GROSA, Giorgio; MASSAROTTI, Alberto; SORBA, Giovanni; CANONICO...espandi
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/1953118
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