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

Author:

de Vos Dick1,Willem Rudolph23,Gielen Marcel2,van Wingerden Kyra E.4,Nooter Kees4

Affiliation:

1. Medical Department, Pharmachemie BV, PO Box 552, Haarlem NL-003 RN, The Netherlands

2. Free University of Brussels VUB, Pleinlaan 2, Department of General and Organic Chemistry, Faculty of Engineering, Brussels B-1050, Belgium

3. Free University of Brussels VUB, Pleinlaan 2, High Resolution NMR Centre HNMR, Brussels B-1050, Belgium

4. Laboratory for Tumor Biology and Pharmacology, Academic Hospital Rotterdam, PO Box 2040, Rotterdam NL-3000 CA, The Netherlands

Abstract

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.

Publisher

Hindawi Limited

Subject

Inorganic Chemistry,Drug Discovery,Pharmacology,Toxicology

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