Unknown

Dataset Information

0

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

Json Xml
altmetric image

Publications

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]

Similar Datasets

Unknown Design, synthesis and structure-activity relationship of 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]furan derivatives as a novel class of inhibitors of tubulin polymerization.
| S-EPMC2762272 | biostudies-literature
Unknown Substituted 2-(3',4',5'-trimethoxybenzoyl)-benzo[b]thiophene derivatives as potent tubulin polymerization inhibitors.
| S-EPMC2922916 | biostudies-literature
Unknown Synthesis and biological evaluation of 2-amino-3-(3',4',5'-trimethoxybenzoyl)-6-substituted-4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives as antimitotic agents and inhibitors of tubulin polymerization.
| S-EPMC2606048 | biostudies-literature
Unknown Synthesis and biological evaluation of 2-aryl-benzimidazole derivatives of dehydroabietic acid as novel tubulin polymerization inhibitors.
| S-EPMC9080489 | biostudies-literature
Unknown Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.
| S-EPMC3172808 | biostudies-literature
Unknown Design and synthesis of novel 5-(4-chlorophenyl)furan derivatives with inhibitory activity on tubulin polymerization.
| S-EPMC6479276 | biostudies-literature
Unknown Synthesis and biological evaluation of novel 5-chloro-<i>N</i>-(4-sulfamoylbenzyl) salicylamide derivatives as tubulin polymerization inhibitors.
| S-EPMC6148682 | biostudies-literature
Unknown Synthesis and antitumor molecular mechanism of agents based on amino 2-(3',4',5'-trimethoxybenzoyl)benzo[b]furan: inhibition of tubulin and induction of apoptosis.
| S-EPMC3190670 | biostudies-literature
Unknown Synthesis, biological evaluation and molecular docking studies of trans-indole-3-acrylamide derivatives, a new class of tubulin polymerization inhibitors.
| S-EPMC4091680 | biostudies-literature
Unknown Synthesis and Molecular Docking Study of New Thiazole Derivatives as Potential Tubulin Polymerization Inhibitors.
| S-EPMC9494671 | biostudies-literature