Synthesis and preliminary cytotoxicity studies of indole-substituted vanadocenes |
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| Authors: | Brendan Gleeson Megan Hogan Helge Müller-Bunz Matthias Tacke |
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| Affiliation: | (1) UCD School of Chemistry and Chemical Biology, Conway Institute of Biomolecular and Biomedical Research, Centre for Synthesis and Chemical Biology (CSCB), University College Dublin, Belfield, Dublin 4, Ireland; |
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| Abstract: | Abstract From the reaction of various 6-indolylfulvenes (1a–1e) with Super Hydride (LiBEt3H), followed by transmetallation with vanadium tetrachloride (VCl4), six indole-substituted vanadocenes; bis-[(1-methylindol-2-yl)methylcyclopentadienyl] vanadium (IV) dichloride (3a), bis-[(1-methyl-5-methoxyindol-2-yl)methylcyclopentadienyl] vanadium (IV) dichloride (3b), bis-[(1-methylindol-3-yl)methylcyclopentadienyl] vanadium (IV) dichloride (3c), bis-[(1-methyl-5-methoxyindol-3-yl)methylcyclopentadienyl] vanadium (IV) dichloride (3d), a dihydrochloride derivative of bis-[(1-methyl-3-dimethylaminomethylindol-2-yl)methylcyclopentadienyl] vanadium (IV) dichloride (3e), and bis-[(1-methyl-5-methoxyindol-3-yl)methylcyclopentadienyl] vanadium (IV) diselenocyanate (3f), were synthesised. The six vanadocenes 3a–f were tested for their cytotoxicity through MTT-based in vitro tests on CAKI-1 cell lines in order to determine their IC50 values. Vanadocenes 3a–f were found to have IC50 values of 48 (±4), 24 (±4), 9.2 (±1.8), 2.5 (±0.8), 2.3 (±0.7) and 22 (±7) μM. |
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