Novel benzyl-substituted vanadocene anticancer drugs |
| |
Authors: | Brendan Gleeson James Claffey Megan Hogan Helge Müller-Bunz Denise Wallis Matthias Tacke |
| |
Institution: | Conway Institute of Biomolecular and Biomedical Research, Centre for Synthesis and Chemical Biology (CSCB), UCD School of Chemistry and Chemical Biology, University College Dublin, Belfield, Dublin 4, Ireland |
| |
Abstract: | From the reaction of 6-(p-methoxyphenyl) fulvene (1a), 6-(3,4-dimethoxyphenyl) fulvene (1b) and 6-(3,4,5-trimethoxyphenyl) fulvene (1c) with LiBEt3H, lithiated cyclopentadienide intermediates (2a–c) were synthesised. These intermediates were then transmetallated to vanadium with VCl4 to yield the benzyl-substituted vanadocenes bis-(p-methoxybenzyl)cyclopentadienyl] vanadium(IV) dichloride (3a), bis-(3,4-dimethoxybenzyl)cyclopentadienyl] vanadium(IV) dichloride (3b), and bis-(3,4,5-trimethoxybenzyl)cyclopentadienyl] vanadium(IV) dichloride (3c). The two vanadocenes 3a and 3c were characterised by single crystal X-ray diffraction. All three vanadocenes had their cytotoxicity investigated through MTT based preliminary in vitro testing on the LLC-PK (pig kidney epithelial) cell line in order to determine their IC50 values and compare them with the corresponding titanocene dichloride derivatives. Vanadocenes 3b–c were found to have IC50 values of 9.1 and 8.3 μM, while 3a showed a superior value of 3.0 μM, respectively. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |
|