Table of Contents
Metal-Based Drugs
Volume 5 (1998), Issue 4, Pages 179-188

The Development of Novel Organotin Anti-Tumor Drugs: Structure and Activity

1Medical Department, Pharmachemie BV, PO Box 552, Haarlem NL-003 RN, The Netherlands
2Free University of Brussels VUB, Pleinlaan 2, Department of General and Organic Chemistry, Faculty of Engineering, Brussels B-1050, Belgium
3Free University of Brussels VUB, Pleinlaan 2, High Resolution NMR Centre HNMR, Brussels B-1050, Belgium
4Laboratory for Tumor Biology and Pharmacology, Academic Hospital Rotterdam, PO Box 2040, Rotterdam NL-3000 CA, The Netherlands

Received 18 June 1998; Accepted 14 July 1998

Copyright © 1998 Hindawi Publishing Corporation. 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.


An overview of the development of anti-tumor organotin derivatives in selected classes of compounds is presented and discussed. High to very high in vitro activity has been found, sometimes equaling that of doxorubicin. Solubility in water is an important issue, dominating the in vivo testing of compounds with promising in vitro properties. The cytotoxicity of the compounds was increased by the presence of a bulky group, an active substituent or one or more polar substituents. Polar substituents may also improve the water solubility. Although organotin derivatives constitute a separate class of compounds, the comparison with cisplatin is inevitable. Among the observed toxicities, neurotoxicity, known from platinum cytostatics, and gastrointestinal toxicity, typical for many oncology drugs, have been detected. Further research to develop novel, useful organotin anti-tumor compounds should be carried out.