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Antitumor properties of some titanocene chalcogenates
Affiliation:1. OsteoRheuma Bern, Bahnhofplatz 1, Bern, Switzerland;2. Department of Rheumatology and Immunology, University Hospital, Bern, Switzerland;3. Institute for Social and Preventive Medicine, University of Bern, Bern, Switzerland;4. Clinical Trial Unit (CTU) Bern, University of Bern, Bern, Switzerland;5. Zentrum für Rheuma- und Knochenerkrankungen, Klinik Im Park, Hirslanden Zürich, Switzerland;1. Université Clermont Auvergne, CNRS, UMR 6324, Clermont-Ferrand, France;2. Foundation for Research and Technology Hellas (FORTH), Heraklion, Crete Greece
Abstract:Five chalcogen-coordinated bis(η5-cyclopentadienyl)titanium(IV) chalcogenolates were tested against fluid Ehrlich ascites tumor for antitumor properties: the titanocene phenolates (C5H5)2TiCl(2,4,6-OC6H2Cl3) (I) and (C5H5)2Ti(OC6F5)2 (II); the titanocene thiophenolate (C5H5)2Ti(SC6F5)2 (III); the titanocene dithiolene chelate (C5H5)2Ti[cis-1,2-S2C2 (CN)2] (IV); and the titanocene selenophenolate (C5H5)2TiCl(SeC6H5) (V). The best antitumor activity and an optimum cure rate of 100% were observed in the case of the pentafluorophenyl derivatives II and III, followed by IV and V which induced cure rates of 90 and 80% respectively. These results confirm that bis(η5-cyclopentadienyl)titanium(IV) diacido complexes can be widely varied at the position of the acido ligands without loss of antitumor potency. The titanocene derivatives described in the present study are the first neutral mercapto and seleno titanocene derivatives for which strong antiproliferative properties have been shown.
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