Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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The Activity of Titanocene T Against Xenografted Caki-1 Tumors

Author(s): Wolfgang Walther, Iduna Fichtner, Anthony Deally, Megan Hogan, Matthias Tacke.

Abstract:

The indole-substituted titanocene dichloride derivative Titanocene T, which is completely water-soluble and shows micromolar activity against the human renal cancer cells Caki-1, was tested in vivo an against xenografted human renal cell tumors in mice. Titanocene T was then given at 25 and 50 mg/kg, seven times every four days during three weeks to two groups (n=6) of Caki-1 tumor-bearing female NMRI:nu/nu mice, while the control group was treated with solvent only. At both doses Titanocene T induced a moderate to good tumor growth reduction with respect to the solventtreated control group, with an optimal T/C value of 51% and 32% and showed neither mortality nor toxicity. Immunohistochemical analysis revealed that the expression of the proliferation marker Ki-67 was reduced in the high-dosage group. Furthermore, anti-angiogenic activity was identified by CD31 staining; the number of micro vessels in a defined tumor area decreased by 27% and 29% due to Titanocene T treatment.

Keywords: Anticancer drug, anti-angiogenic drug, Titanocene, Renal cell cancer, Xenograft

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Article Details

VOLUME: 10
ISSUE: 5
Year: 2013
Page: [375 - 381]
Pages: 7
DOI: 10.2174/1570180811310050002
Price: $58