Ontology highlight
ABSTRACT:
SUBMITTER: La Regina G
PROVIDER: S-EPMC3261769 | biostudies-literature | 2011 Dec
REPOSITORIES: biostudies-literature
Journal of medicinal chemistry 20111121 24
New arylthioindoles (ATIs) were obtained by replacing the 2-alkoxycarbonyl group with a bioisosteric 5-membered heterocycle nucleus. The new ATIs 5, 8, and 10 inhibited tubulin polymerization, reduced cell growth of a panel of human transformed cell lines, and showed higher metabolic stability than the reference ester 3. These compounds induced mitotic arrest and apoptosis at a similar level as combretastatin A-4 and vinblastine and triggered caspase-3 expression in a significant fraction of cel ...[more]