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;TRAVELLI, Cristina;APRILE, SILVIO;TORRETTA, SIMONE;GROSA, Giorgio;MASSAROTTI, Alberto;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.File in questo prodotto:
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