TY - JOUR
T1 - Design, synthesis, and biological evaluation of combretabenzodiazepines
T2 - A novel class of anti-tubulin agents
AU - Galli, Ubaldina
AU - Travelli, Cristina
AU - Aprile, Silvio
AU - Arrigoni, Elena
AU - Torretta, Simone
AU - Grosa, Giorgio
AU - Massarotti, Alberto
AU - Sorba, Giovanni
AU - Canonico, Pier Luigi
AU - Genazzani, Armando A.
AU - Tron, Gian Cesare
N1 - Publisher Copyright:
© 2015 American Chemical Society.
PY - 2015/2/12
Y1 - 2015/2/12
N2 - 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.
AB - 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.
UR - http://www.scopus.com/inward/record.url?scp=84922769004&partnerID=8YFLogxK
U2 - 10.1021/jm5016389
DO - 10.1021/jm5016389
M3 - Article
SN - 0022-2623
VL - 58
SP - 1345
EP - 1357
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 3
ER -