Antitumour Organometallics. III. In Vivo Activity of Diphenylantimony(III) and Diorganotin(IV) Dithiophosphorus Derivatives Against P388 Leukemia

Bernhard K Keppler,Cristian Silvestru,Ionel Haiduc

doi:10.1155/mbd.1994.73

Bernhard K Keppler, Cristian Silvestru + Show 1 more

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https://doi.org/10.1155/mbd.1994.73

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Abstract

Diphenylantimony(III) and diorganotin(IV) derivatives of dithiophosphorus ligands, i.e. Ph2SbS2PR′2 (R′ = Ph, OPr-i) and R2Sn(S2PR′2)2 (R = n-Bu, Ph, R′ = Ph; R = Ph, R′ = OPr-i), have been screened against P388 leukemia in mice. All the compounds showed marginal activity towards this tumor system, some of them increasing the life span of the animals with more than 20%. The best results were obtained with (di-iso-propylphosphorodithioato)diphenylantimony(III) which exhibited a T/C value of 136%, at a dose of 5 mg/kg, administered on days 1,2 and 3 after tumor transplantation.

Highlights

In recent years, the potential antitumor activity of organometallics, i.e. compounds containing direct metal-carbon bonds, has received an increased attention, since more and more derivatives of either transition and Main Group metals were found to exhibit interesting inhibitory properties on animal tumor systems
Among Main Group metal compounds, organotin(IV) derivatives occupy a top position related to their antitumor effects, with some of them being even more active than cisplatin in in vitro tests.[2,3,4,5,6,7,8,9]
Interest in organoantimony(lll) compounds as potential antitumor agents arose in recent years when diphenylantimony(lll) derivatives of dithiophosphorus ligands were reported as the first organoantimony compounds to exhibit antitumor properties in vitro and in vivo against Ehrlich ascites tumor.[10,11,12]

Summary

INTRODUCTION

The potential antitumor activity of organometallics, i.e. compounds containing direct metal-carbon bonds, has received an increased attention, since more and more derivatives of either transition and Main Group metals were found to exhibit interesting inhibitory properties on animal tumor systems. N-Bu2Sn(S2PPh2)[2], was included in the screening, since a lot of previous reports concerning the antitumor activity of organotins[5,8,9] have suggested that the presence of the di-n-butyltin moiety improve the in vitro inhibitory effects against human tumor cell lines (MCF-7 and WiDr) in comparison to analogous compounds containing phenyl groups bound to tin A dibutyltin(IV) derivative, L e. n-Bu2Sn(S2PPh2)[2], was included in the screening, since a lot of previous reports concerning the antitumor activity of organotins[5,8,9] have suggested that the presence of the di-n-butyltin moiety improve the in vitro inhibitory effects against human tumor cell lines (MCF-7 and WiDr) in comparison to analogous compounds containing phenyl groups bound to tin

MATERIALS AND METHODS

RESULTS AND DISCUSSION

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