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Diheteroarylmethyl substituted titanocenes: a novel class of possible anti-cancer drugs

Pampillon, C., Sweeney, N.J., Strohfeldt, K. and Tacke, M. (2006) Diheteroarylmethyl substituted titanocenes: a novel class of possible anti-cancer drugs. Inorganica Chimica Acta, 359 (12). pp. 3969-3975. ISSN 0020-1693

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To link to this article DOI: 10.1016/j.ica.2006.05.021

Abstract/Summary

From the reaction of tert-butyl lithium or n-butyl lithium with N-methylpyrrole (1a), furan (1b) or 2-bromo-thiophen (1c), 2-N-methylpyrrolyl lithium (2a), 2-furyl lithium (2b) or 2-thiophenyl lithium (2c), respectively, was obtained. When reacted with 6-(2-N-methylpyrrolyl) fulvene (3a), 6-(2-furyl) fulvene (3b) or 6-(2-thiophenyl) fulvene (3c), the corresponding lithiated intermediates were formed (4a-c). Titanocenes (5a-c) were obtained through transmetallation with titanium tetrachloride. When these titanocenes were tested against pig kidney epithelial (LLC-PK) cells, inhibitory concentrations (IC50) of 32 mu M, 140 mu M, and 240 mu M, respectively, were observed. These values represent improved cytotoxicity against LLC-PK, compared to their ansa-analogues. (c) 2006 Elsevier B.V. All rights reserved.

Item Type:Article
Refereed:Yes
Divisions:Faculty of Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy
ID Code:13661
Uncontrolled Keywords:anti-cancer drug, cis-platin, titanocene, fulvene, carbolithiation, LLC-PK, tert-butyl lithium , TITANIUM DICHLORIDE, ORGANIC-CHEMISTRY, ANSA-TITANOCENES, FULVENES, COMPLEXES, DERIVATIVES, METALLOCENES, CISPLATIN, AGENTS, TRIAL

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