Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
Molecules that target microtubules have an important role in the treatment of cancer. A new class of inhibitors of tubulin polymerization based on the 2-(3,4,5-trimethoxybenzoyl)-2-dimethylamino-benzo[b]furan molecular skeleton was synthesized and evaluated for antiproliferative activity, inhibition of tubulin polymerization, and cell cycle effects. The most promising compound in this series was 2-(3,4,5-trimethoxybenzoyl)-3-dimethylamino-6-methoxy-benzo[b]furan, which inhibits cancer cell growth at nanomolar concentrations and interacts strongly with tubulin by binding to the colchicine site.
Romagnoli
Romeo
R
Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy. rmr@unife.it <rmr@unife.it>
Baraldi
Pier Giovanni
PG
Sarkar
Taradas
T
Carrion
Maria Dora
MD
Cruz-Lopez
Olga
O
Lopez Cara
Carlota
C
Tolomeo
Manlio
M
Grimaudo
Stefania
S
Di Cristina
Antonietta
A
Pipitone
Maria Rosaria
MR
Balzarini
Jan
J
Gambari
Roberto
R
Ilaria
Lampronti
L
Saletti
Roberto
R
Brancale
Andrea
A
Hamel
Ernest
E