Metal-Based Drugs 
Volume 5 (1998), Issue 2, Pages 83-90
doi:10.1155/MBD.1998.83

Toxicity Profiles In Vivo in Mice and Antitumour Activity in Tumour-Bearing Mice of Di- and Triorganotin Compounds

M. Gielen,1 R. Willem,1,2 H. Dalil,1 D. de Vos,3 C. M. Kuiper,4 and G. J. Peters4

 1Free University of Brussels VUB, Faculty of Applied Sciences, Room 8G512, Pleinlaan 2, Brussels B-1050, Belgium
2Free University of Brussels VUB, High Resolution NMR Centre, Pleinlaan 2, Brussels B-1050, Belgium
3Medical Department, Pharmachemie B. V., Haarlem, The Netherlands
4Department of Oncology, Laboratory of Biochemical Pharmacology, University Hospital VU, de Boelelaan 1117, Amsterdam NL- 1081 HV, The Netherlands
Received 21 January 1998; Accepted 12 February 1998

Abstract

The in vivo toxicity profiles in mice and the antitumour activity in tumour bearing mice were screened for four di-n-butyltin and five triorganotin carboxylates, di-n-butyltin diterebate (5), bis(phenylacetate) (6), bis(deoxycholate) (7), bis(lithocholate) (8), tri-n-butyltin terebate (9), cinnamate (10), and triphenyltin terebate (11).

At their maximum tolerated dosis (MTD), no antitumour effect (T/C ~1) was observed for the compounds 5, 7, 9, 10 and 11. The compounds 6 (T/C = 0.51) and 8 (T/C = 0.42) showed clear antitumour activity after single dose administration and might therefore be of interest for further antitumour activity studies.