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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.

SUBMITTER: Romagnoli R 

PROVIDER: S-EPMC2574800 | biostudies-literature | 2008 Sep

REPOSITORIES: biostudies-literature

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Synthesis and biological evaluation of 2-(3',4',5'-trimethoxybenzoyl)-3-N,N-dimethylamino benzo[b]furan derivatives as inhibitors of tubulin polymerization.

Romagnoli Romeo R   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  

Bioorganic & medicinal chemistry 20080817 18

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 growt  ...[more]

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