title: Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.
abstract: 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.
authors.affiliation: Dipartimento di Scienze Farmaceutiche, Università di Ferrara, Via Fossato di Mortara 17-19, 44100 Ferrara, Italy. rmr@unife.it <rmr@unife.it>
authors.forename: Romeo
authors.initials: R
authors.lastname: Romagnoli
authors.forename: Pier Giovanni
authors.initials: PG
authors.lastname: Baraldi
authors.forename: Taradas
authors.initials: T
authors.lastname: Sarkar
authors.forename: Maria Dora
authors.initials: MD
authors.lastname: Carrion
authors.forename: Olga
authors.initials: O
authors.lastname: Cruz-Lopez
authors.forename: Carlota
authors.initials: C
authors.lastname: Lopez Cara
authors.forename: Manlio
authors.initials: M
authors.lastname: Tolomeo
authors.forename: Stefania
authors.initials: S
authors.lastname: Grimaudo
authors.forename: Antonietta
authors.initials: A
authors.lastname: Di Cristina
authors.forename: Maria Rosaria
authors.initials: MR
authors.lastname: Pipitone
authors.forename: Jan
authors.initials: J
authors.lastname: Balzarini
authors.forename: Roberto
authors.initials: R
authors.lastname: Gambari
authors.forename: Lampronti
authors.initials: L
authors.lastname: Ilaria
authors.forename: Roberto
authors.initials: R
authors.lastname: Saletti
authors.forename: Andrea
authors.initials: A
authors.lastname: Brancale
authors.forename: Ernest
authors.initials: E
authors.lastname: Hamel