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Bioinorganic Chemistry and Applications
Volume 2009, Article ID 908625, 8 pages
http://dx.doi.org/10.1155/2009/908625
Research Article

Synthesis and Evaluation of Novel Organogermanium Sesquioxides As Antitumor Agents

1State Key Laboratory of Natural and Biomimetic Drugs, Peking University Health Science Center, Beijing 100083, China
2Department of Nuclear Medicine, Peking University First Hospital, Beijing 100034, China
3Department of Chemistry, Beijing Normal University, Beijing 100875, China

Received 7 October 2008; Revised 16 December 2008; Accepted 6 February 2009

Academic Editor: Anastasios Keramidas

Copyright © 2009 Chun Li Zhang et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

Abstract

Five new organogermanium sesquioxides have been synthesized and characterized by elemental analysis and IR spectra. All the compounds were tested for antitumor activities against KB, HCT, and Bel cells in vitro. Compound 5 ( 𝛾 -thiocarbamido propyl germanium sesquioxide) showed excellent antitumor activity, and its inhibition yield to KB, HCT, and Bel cells was 92.9%, 84.9%, and 70.9%, respectively. A rapid method was described for the labeling compound 5 with 9 9 m T c , and the optimum labeling conditions were investigated. The labeling yield is above 90% in pH 7.0, 2 0 C , reaction time greater than 10 minutes, 1 mg of compound 5, and 0.075 0.1 mg of S n C l 2 . The biodistribution of 9 9 m T c labeled compound 5 in nude mice bearing human colonic xenografts was studied. The result showed that the tumor uptakes were 0.73, 0.97, 0.87, and 0.62 ID%/g at 1-hour, 3-hour, 6-hour, and 20-hour postinjection, respectively. T/NT (the uptake ratio for per gram of tumor over normal tissues) was 18.3 for tumor versus brain and 5.81 for tumor versus muscle at 20-hour postinjection. The tumor clearance was slow. The results showed that compound 5 may be developed to be a suitable cancer therapeutic agent.