Abstract
From the novel reaction of Super Hydride (LiB(Et) 3H) with 6-( p- N, N-dimethylanilinyl)fulvene ( 1a) or 6-( p-methoxyphenyl)fulvene ( 1b) the corresponding lithium cyclopentadienide intermediates ( 2a, 2b) were obtained. When reacted with TiCl 4, bis-[( p-dimethylaminobenzyl)cyclopentadienyl]titanium (IV) dichloride ( 3a) and bis-[( p-methoxybenzyl)cyclopentadienyl]titanium (IV) dichloride ( 3b) were obtained. Titanocene 3a was reacted with an ethereal solution of HCl, by which its dihydrochloride derivative ( 3c) was formed and isolated. Titanocenes 3b and 3c were characterised by X-ray crystallography. When the titanocenes 3a– c were tested against pig kidney carcinoma (LLC-PK) cells inhibitory concentrations (IC 50) of 1.2 × 10 −4 M, 2.1 × 10 −5 M and 9.0 × 10 −5 M, respectively, were observed. These values represent improved cytotoxicity against LLC-PK, most notably for 3b (Titanocene Y), which is a hundred times more cytotoxic than titanocene dichloride itself.
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