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Synthesis and cytotoxicity studies of new dimethylamino-functionalised and aryl-substituted titanocene anti-cancer agents

Pampillon, C., Claffey, J., Strohfeldt, K. and Tacke, M. (2008) Synthesis and cytotoxicity studies of new dimethylamino-functionalised and aryl-substituted titanocene anti-cancer agents. European Journal of Medicinal Chemistry, 43 (1). pp. 122-128. ISSN 0223-5234

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To link to this item DOI: 10.1016/j.ejmech.2007.02.011

Abstract/Summary

From the carbolithiation of 6-N,N-dimethylamino fulvene (3a) and different lithiated aryl species [p-N,N-dimethylanilinyl lithium, p-anisyl lithium and 4-lithio-benzo[1.3]dioxole (2a-c)], the corresponding lithium cyclopentadienide intermediates 4a-c were formed. These three lithiated intermediates underwent a transmetallation reaction with TiCl4 resulting in dimethylamino-functionalised and aryl-substituted titanocenes 5a-c. When these titanocenes were tested against LLC-PK cells, the IC50 values obtained were of 54, 45 and 26 mu M for titanocenes 5a, b and c, respectively. The most cytotoxic titanocene in this paper, 5c is approximately 10 times less cytotoxic than cis-platin, which showed an IC50 value of 3.3 mu M, when tested on the LLC-PK cell line, but approximately 100 times better than titanocene dichloride. (C) 2007 Elsevier Masson SAS. All rights reserved.

Item Type:Article
Refereed:Yes
Divisions:Faculty of Life Sciences > School of Chemistry, Food and Pharmacy > School of Pharmacy
ID Code:13663
Uncontrolled Keywords:anti-cancer agents, cis-platin, titanocene, fulvene, dimethylamino-functionalised metallocenes, LLC-PK , TITANIUM DICHLORIDE, ANTITUMOR-ACTIVITY, ANSA-METALLOCENES, COLORECTAL-CANCER, ORGANIC-CHEMISTRY, DRUGS, FULVENES, COMPLEXES, CISPLATIN, TUMOR

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