Synthesis and preliminary cytotoxicity studies of achiral pyrrolyl-substituted titanocenes |
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Authors: | Anthony Deally,James ClaffeyBrendan Gleeson,Megan HoganHelge Mü ller-Bunz,Siddappa PatilDonal F. O&rsquo Shea,Matthias Tacke |
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Affiliation: | UCD School of Chemistry and Chemical Biology, Centre for Synthesis and Chemical Biology (CSCB), Conway Institute of Biomolecular and Biomedical Research, University College Dublin, Belfield, Dublin 4, Ireland |
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Abstract: | From the reaction of various 6-pyrrolylfulvenes (3a–3d) with Super Hydride (LiBEt3H), lithiated cyclopentadienide intermediates (4a–4d) were synthesised. These intermediates were then transmetallated with titanium tetrachloride TiCl4 to yield the pyrrolyl-substituted titanocenes bis-[((1-(4-methoxybenzyl)-pyrrole)2-)cyclopentadienyl]titanium(IV) dichloride (5a), bis-[((1-(4-methoxyphenyl)-pyrrole)2-)cyclopentadienyl]titanium(IV) dichloride (5b), bis-[((2,4-bis(4-methoxyphenyl)-1-methyl-pyrrole)2-)cyclopentadienyl]titanium(IV) dichloride (5c), bis-[((2-(4-methoxyphenyl)-1-methyl-pyrrole)2-)cyclopentadienyl]titanium(IV) dichloride (5d). Titanocene 5b crystallised and was characterised by X-ray crystallography. The four titanocenes 5a–5d were tested for their cytotoxicity through MTT-based in vitro tests on CAKI-1 cell lines in order to determine their IC50 values. Titanocenes 5a–5d were found to have IC50 values of 440 (±35), 68 (±14), 105 (±30), and 36 (±7) μM. |
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Keywords: | Anticancer drug Titanocene dichloride Pyrrole Renal-cell cancer CAKI-1 Cytotoxicity |
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