Metal-Based Drugs 
Volume 5 (1998), Issue 4, Pages 189-196
doi:10.1155/MBD.1998.189

Synthesis, Characterization and In Vitro Antitumour Activity of Di-n-Butyl, Tri-n-Butyl and Triphenyltin 3,6-Dioxaheptanoates and 3,6,9-Trioxadecanoates

Martine Kemmer,1 Marcel Gielen,1,2 Monique Biesemans,2,3 Dick de Vos,4 and Rudolph Willem2,3

 1Université Libre de Bruxelles, Service de Chimie Organique, Av. F. D. Roosevelt, 50, Bruxelles B-1050, Belgium
2Free University of Brussels VUB, Pleinlaan 2, AOSC Unit, Faculty of Applied Sciences, Brussel B-1050, Belgium
3Free University of Brussels VUB, Pleinlaan 2, High Resolution NMR Center HNMR, Brussel B-1050, Belgium
4Medical Department, Pharmachemie B. V., Haarlem NL-2003 RN, The Netherlands
Received 23 June 1998; Accepted 14 July 1998

Abstract

A series of di- and triorganotin 3,6-dioxaheptanoates and 3,6,9-trioxadecanoates were synthesized and characterized by H1, C13 and S117n NMR, electrospray mass and S119mn Mössbauer spectroscopy, as well as elemental analysis. Their in vitro antitumour activity against seven tumoural cell lines of human origin, two breast cancers (MCF-7, EVSA-T), a colon carcinoma (WiDr), an ovarian cancer (IGROV), a melanoma (M 19 MEL), a renal cancer (A 498) and a non small cell lung cancer (H 226), is reported. They are characterized by similar inhibition doses ID50 as the analogous di- and triorganotin derivatives of 4-carboxybenzo-15-crown-5 and -18-crown-6 and in some cases by much lower ID50 values than clinically used reference compounds such as doxorubicine and methotrexate.